Inhibitor clinical compound 2. Medical search. Frequent questions

The US Department of Defense developed favipiravir in partnership with MediVector, Inc. as a broad-spectrum antiviral and sponsored it through FDA Phase II and Phase III clinical trials, where it demonstrated safety in humans and efficacy against the influenza virus. (wikipedia.org)
As of May 2021[update], large-cohort clinical trials are underway. (wikipedia.org)
Fibroblast growth factor receptors (FGFR) 2 and 3 have been established as drivers of numerous types of cancer with multiple drugs approved or entering late stage clinical trials. (rcsb.org)
Systematic reviews of clinical trials suggest that the overall efficacy of DPP-4 inhibitors in patients with type 2 diabetes generally is similar. (nih.gov)
The study has been approved for clinical trials in the United States, Australia, South Korea and other countries and regions. (tmcnet.com)
At present, clinical trials conduction and commercialization preparations of Senaparib for various indications in mainland China, Hong Kong and Macau are being performed by a joint venture company established by IMPACT Therapeutics and Junshi Biosciences. (tmcnet.com)
We want to make HIF-2 inhibitors available to patients and are currently carrying out clinical trials," said Dr. James Brugarolas, Director of the Kidney Cancer Program, who is leading an $11 million SPORE grant from the National Cancer Institute seeking to translate new discoveries into novel therapies for kidney cancer patients. (eurekalert.org)
I look forward to the results of future clinical trials. (biospace.com)
The robustness of the screen was assessed by the identification of drugs, such as Chloroquine derivatives and protease inhibitors, already in clinical trials. (biorxiv.org)
This article reviews current anticancer small-molecule inhibitors targeting epigenetic modified enzymes and displays their performances in different stages of clinical trials. (frontiersin.org)
At present, there are no specific RET inhibitors in clinical trials. (esmo.org)
RET inhibitors in phase II trials are active in a subgroup of patients with RET-rearranged NSCLC with lower RR to that observed in EGFR-mutant/ALK patients. (esmo.org)
Ongoing/planned clinical trials include testing of apatinib, cabozantinib, ponatinib, and alectinib in that patient population. (esmo.org)
Current autophagy-modulating compounds in clinical trials are also summarized. (nature.com)
ECHO and THRIVE are two pivotal Phase 3 clinical trials which evaluated the efficacy and safety of rilpivirine in 1,368 antiretroviral treatment-naïve HIV-1-infected adults with plasma HIV-1 RNA ≥ 5000 copies/mL. (jnj.com)
Clinical trials have shown that patients with prostate, lung, and basal cell carcinoma have benefited from treatment with itraconazole, and there are additional reports of activity in leukaemia, ovarian, breast, and pancreatic cancers. (ecancer.org)
GlobalData's clinical trial report, "Pancreatic Cancer Global Clinical Trials Review, H1, 2016' provides an overview of Pancreatic Cancer clinical trials scenario. (globaldata.com)
This report provides top line data relating to the clinical trials on Pancreatic Cancer. (globaldata.com)
The report offers coverage of disease clinical trials by region, country (G7 & E7), phase, trial status, end points status and sponsor type. (globaldata.com)
GlobalData Clinical Trial Reports are generated using GlobalData's proprietary database - Pharma eTrack Clinical trials database. (globaldata.com)
Clinical trials are collated from 80+ different clinical trial registries, conferences, journals, news etc across the globe. (globaldata.com)
Clinical trials database undergoes periodic update by dynamic process. (globaldata.com)
Attributes of the drug, company and its clinical trials play a fundamental role in drug-specific PTSR and likelihood of approval. (pharmaceutical-technology.com)
Astex Pharmaceuticals is also advancing several of its compounds into clinical trials in collaboration with Novartis, AstraZeneca, GSK, and Janssen. (pharmaceutical-technology.com)
The most commonly reported adverse reactions from clinical trials are fatigue, malaise, hypotension, and dizziness. (nih.gov)
Indotecan (LMP400) and indimitecan (LMP776) are being studied in Phase I clinical trials, and one of these two agents may be promoted to a Phase II trial in the future. (purdue.edu)
As the three agents enter into and progress through clinical trials, increasing supplies of the drugs will be required to support their studies. (purdue.edu)
The EU Clinical Trials Register currently displays 43723 clinical trials with a EudraCT protocol, of which 7255 are clinical trials conducted with subjects less than 18 years old. (clinicaltrialsregister.eu)
Because most Coccidioides infections resolve without specific therapy, few clinical trials have assessed outcomes in less-severe disease. (medscape.com)
Clinical trials are currently investigating agents, such as AP13573 and ET743 (trabectedin), in patients with advanced leiomyosarcomas, liposarcomas , or osteosarcomas . (medscape.com)
Paromomycine, an aminoglycoside, has been tested as a topical ointment for the possible treatment of CL but more clinical trials are needed against the main parasite causing CL [4]. (who.int)
Often, a drug that is efficacious in clinical trials is not very effective in actual use. (msdmanuals.com)
In such cases, clinical trials would need to be very large and run for a long time unless a surrogate outcome (eg, lowered blood pressure) is used. (msdmanuals.com)
Parasites were topical ointment for the possible treatment grown to a density of 5 ×107 parasites/mL, of CL but more clinical trials are needed spun down, reconstituted in Medium 199 against the main parasite causing CL [ 4 ]. (who.int)
Treatment with neuraminidase inhibitors has been shown to have clinical and public health benefit in reducing illness and severe outcomes of influenza based on evidence from randomized controlled trials, meta-analyses of randomized controlled trials, and observational studies during past influenza seasons and during the 2009 H1N1 pandemic. (cdc.gov)

In this review, we summarize the basic principles manipulating the abovementioned epigenetic pathways and highlight the evidence of the promising clinical and preclinical results using small-molecule inhibitors against chromatin regulators for cancer treatment. (frontiersin.org)
5 3 Herein, we have developed and performed a targeted small molecule screen to identify compounds which downregulate α-globin expression. (haematologica.org)
The small molecule compound, Erlotinib is a receptor tyrosine kinase inhibitor (EGFR antagonist) and belongs to molecular targeted therapy Drugs. (lookchem.com)

OPV to prevent the risk for vaccine-associated paralytic have been reported as potent inhibitors of the replication of picornaviruses in vitro ( 8 ). (cdc.gov)
With the exception of the primary hydroxylated metabolite of saxagliptin, which is 2-fold less potent than its parent molecule, metabolic products of hepatic biotransformation are minimally active and none appreciably contribute to either the therapeutic or the toxic effects of DPP-4 inhibitors. (nih.gov)
HM71224 is a potent and effective BTK inhibitor and has successfully demonstrated proof of mechanism in preclinical studies and a Phase 1 study in Europe,' said Dr. Gwan Sun Lee, president and CEO of Hanmi Pharmaceutical, in a press release. (drugdiscoverynews.com)
Many potent RET inhibitor compounds have been initially designed to target other tyrosine kinase. (esmo.org)
We have shown that this compound has potent anti-leishmanial activity in vitro [6]. (who.int)

The recent emergence of SARS-CoV-2 Omicron (B.1.1.529 lineage) variants possessing numerous mutations has raised concerns of decreased effectiveness of current vaccines, therapeutic monoclonal antibodies and antiviral drugs for COVID-19 against these variants 1 , 2 . (nature.com)
In addition, we found that some therapeutic monoclonal antibodies (REGN10987 plus REGN10933, COV2-2196 plus COV2-2130, and S309) and antiviral drugs (molnupiravir, nirmatrelvir and S-217622) can restrict viral infection in the respiratory organs of BA.2-infected hamsters. (nature.com)
These findings suggest that the replication and pathogenicity of BA.2 is similar to that of BA.1 in rodents and that several therapeutic monoclonal antibodies and antiviral compounds are effective against Omicron BA.2 variants. (nature.com)
In addition, we evaluated the efficacy of therapeutic monoclonal antibodies and antiviral drugs for COVID-19 against BA.2 variants in vivo. (nature.com)
Senaparib's preliminary clinical data demonstrated superior tolerability and wider therapeutic window compared to other marketed PARP inhibitors, showing the best-in-class potential. (tmcnet.com)
Senaparib's preliminary clinical data demonstrated superior tolerability and wider therapeutic window compared with other PARPi. (tmcnet.com)
Supuran, C.T. and Scozzafava, A. (2000) Carbonic Anhydrase Inhibitors and Their Therapeutic Potential. (scirp.org)
The hits were sorted according to their chemical composition and their known therapeutic effect, then EC50 and CC50 were determined for a subset of compounds. (biorxiv.org)
Targeting of the fibroblast activation protein is currently being explored for different tumor entities using PET imaging with the fibroblast activation protein inhibitor (FAPI) 68 Ga-FAPI-04, and the first therapeutic applications of 90 Y-FAPI-04 have been applied. (snmjournals.org)
Unexpectedly, and despite our optimization efforts, the prodrug of 26 still possesses a therapeutic window insufficient to support further clinical development. (rcsb.org)
The aim of this workshop was to assess the progress that has been made over the past 2 years in bringing effective therapeutic protocols that use agents capable of reverting pathologic epigenetic changes into the clinic. (aacrjournals.org)
Such libraries are used for screening against therapeutic targets in order to find hit compounds that may be further developed into drugs and/or used as research tools to better understand the underlying biology and its relevance to pharmacological intervention. (ddw-online.com)
Sahdeo Prasad, Amit Kumar Tyagi , " Cancer Preventive and Therapeutic Compounds: Gift From Mother Nature ", Bentham Science Publishers (2017). (benthamscience.com)
The therapeutic agent 2-(2-nitro-4-trifluoromethylbenzoyl)-1,3-cyclohexanedione (NTBC) interrupts the pathway after formation of 4-OH-phenylpyruvic acid. (medscape.com)
[ 6 ] As of yet, PDE11 inhibition with therapeutic doses of tadalafil has shown no clinical significance. (medscape.com)

To develop dual acting BRD4-kinase inhibitors, a kinase inhibitor library was screened to identify compounds with binding potential for the acetyl-lysine binding site of BRD4. (moffitt.org)
Imatinib mesylate (Gleevec), a 2-phenylaminopyridine that functions as a tyrosine kinase inhibitor, targets the c-kit domain expressed by some GISTs . (medscape.com)

Most experience with nevirapine is in combination with nucleoside reverse transcriptase inhibitors (NRTIs). (who.int)

Previously, Hanmi was able to demonstrate the compound's safety and efficacy in a clinical trial of lung cancer patients who had developed resistance to conventional anticancer drugs. (drugdiscoverynews.com)
The evidence for these anticancer effects, in vitro , in vivo , and clinical are summarised, and the putative mechanisms of their action outlined. (ecancer.org)
Three compounds discovered in the Cushman laboratory are under investigation in humans and canines as potential anticancer drugs. (purdue.edu)

In these patients, no protease inhibitor resistance was detected, meaning further combination therapy with protease inhibitors could remain a viable treatment option for those experiencing virologic failure with darunavir monotherapy. (jnj.com)
But you can suppress the failure by using a protease inhibitor combination. (theseoultimes.com)
And we do have now, Cabotegravir single tablet protease inhibitor combination that can be used if one fails on Cabotegravir/ Rilpivirine, said Orkin. (theseoultimes.com)

When only 1 or a few of antipicornavirus drugs for their ability to inhibit PV rep- compounds had been described for a particular target (for lication in vitro. (cdc.gov)
No DPP-4 inhibitor has been shown to inhibit or to induce hepatic CYP-mediated drug metabolism. (nih.gov)
Our technology is a family of orally bioavailable small molecules that inhibit BRD4 with activities equivalent to that of the prototypical BRD4 inhibitor JQ1. (moffitt.org)
In addition to inhibiting BRD4 at an IC50 of at least 4 nM, our compounds also potently inhibit the protein kinases JAK2 and FLT3, and they have IC50s for JAK2 that are comparable to those of the JAK2 inhibitors currently in the clinic and on the market. (moffitt.org)
Lastly, PDE5 inhibitors (e.g., tadalafil) are commonly used in order to treat ED as well as inhibit PDE11, which is found in the prostate and testes. (medscape.com)

Here, we summarize the different types of epigenetic enzymes which target corresponding protein domains, emphasize DNA methylation , histone modifications, and microRNA-mediated cooperation with epigenetic modification, and highlight recent achievements in developing targets for epigenetic inhibitor therapy. (frontiersin.org)
This identified IOX1, a pan-histone demethylase inhibitor, which selectively downregulates α-globin expression without perturbing erythroid differentiation or general gene expression, more specifically β-like globin expression. (haematologica.org)
The code is an array of post-translational modifications (acetylation, phosphorylation, methylation, ubiquitination, and sumoylation) of NH 2 -terminal tails of core histone and to a lesser degree their globular domains. (aacrjournals.org)
Histone hyperacetylation and H3K4 methylation are associated with unmethylated DNA, euchromatin, and gene expression ( Fig. 2 ). (aacrjournals.org)

OSAKA, Japan & CAMBRIDGE, Mass.--( BUSINESS WIRE )-- Takeda ( TSE:4502/NYSE:TAK ) today announced positive results from a Phase 2b clinical trial of TAK-279 (NDI-034858), a highly selective, oral allosteric tyrosine kinase 2 (TYK2) inhibitor, in patients with moderate-to-severe plaque psoriasis. (biospace.com)
Hochberg, M.C. (2005) COX-2 Selective Inhibitors in the Treatment of Arthritis: A Rheumatologist Perspective. (scirp.org)
Our data show that selective silencing of α-globin expression in erythroid cells is pharmacologically feasible, and IOX1 is a lead compound to developing new therapy to treat β-thalassemia through the novel pathway of downregulating α-globin expression. (haematologica.org)
It is also running an R&D programme aimed at identifying one or more selective S1P-1 agonist compounds to advance into clinical testing. (pharmatimes.com)

By providing new information on molecules inhibiting SARS-CoV-2 replication in vitro , this study could contribute to the short-term repurposing of drugs against Covid-19. (biorxiv.org)
Moreover, we show that apabetalone inhibits SARS-CoV-2 infection in vitro to levels comparable to antiviral agents. (biorxiv.org)

DPP-4 inhibitors are readily absorbed orally. (nih.gov)
Lead compounds are orally bioavailable with favorable PK/PD properties in mice. (moffitt.org)
Praecis has a MetAP-2 inhibitor, PPI-2458, in clinical development for cancer indications, including non-Hodgkin's lymphoma and solid tumours, and what it describes as "an innovative drug discovery technology," DirectSelect, which enables the generation and practical use of ultra-large libraries for the discovery of orally active compounds. (pharmatimes.com)

Antiviral agents do not confer ecules that have previously been reported to be inhibitors immunity but could be used prophylactically as well as of picornavirus replication and discuss their potential use, therapeutically. (cdc.gov)

Traditionally, proteins like HIF-2 were disregarded as drug targets because their shape made it nearly impossible to design drugs against them," Dr. Brugarolas said. (eurekalert.org)
After 2 decades of rapid development in theranostics, a variety of new targets are available for further clinical investigation. (snmjournals.org)
For two decades or more, the rate at which drugs against new targets are launched has been relatively constant but the rate of developing drugs against completely new classes of drug target has been significantly lower (2). (ddw-online.com)
Target-focused compound libraries have been a key enabling component of the tool kit opening up kinase drug discovery, consisting of collections of compounds designed to interact with a family of related kinase targets (4). (ddw-online.com)
Mulitkinase inhibitor that targets several tyrosine kinase inhibitors implicated in tumor growth, pathologic angiogenesis, and metastatic progression. (medscape.com)

The unique aspect of this report lies in the example, with enviroxime, the sole protein 3A-targeting fact that 1) certain drugs (e.g., rupintrivir) were specifi cally drug reported so far), the impact in the clinical setting was developed to treat rhinovirus and other infections and have considered less important. (cdc.gov)
DALLAS - September 05, 2016 -A new class of drugs called HIF-2 inhibitors is more effective and better tolerated than the standard of care drug sunitinib in treating kidney cancer, researchers with the Kidney Cancer Program at Harold C. Simmons Comprehensive Cancer Center have found. (eurekalert.org)
In the Nature study, researchers compared the two drugs head to head and found that the HIF-2 inhibitor was more active than sunitinib and that it was active against tumors progressing on sunitinib. (eurekalert.org)
Epigenetic drugs show significant effects on both preclinical and clinical studies in which the target development and research offer a promising direction for cancer therapy. (frontiersin.org)
Tyrosine kinase inhibitors (TKIs) are the drugs of choice for initial therapy of CML. (medscape.com)
Clinical consideration for BPH should include the elements of male sexual function, patients' age, and the characteristics and comprehensive effects of each group of drugs. (medscape.com)
While antiviral drugs work best when treatment is started within 2 days of illness onset, clinical benefit has been observed even when treatment is initiated later. (cdc.gov)

Inorganic arsenic compounds have been used as pesticides, but can no longer be used in agriculture. (cdc.gov)
Some organic arsenic compounds may be used as pesticides or as additives in animal feed. (cdc.gov)

JAK2-driven cells show no resistance to dual inhibitors, while the same cells develop rapid resistance to Ruxolitinib and Fedratinib. (moffitt.org)
Islatravir is a nucleoside transcription translocation inhibitor, it has a long half life, inhibits viral replication, and its multiple mechanisms of action contribute to its high potency and high barrier to resistance, including drug resistant viruses. (theseoultimes.com)
During the last 2 decades, many attempts have been made to develop effective new compounds for treating cutaneous leishmaniasis (CL) that would be economical, that could be applied topically to lesions and that would avoid the development of resistance. (who.int)
The choice of a subsequent therapy after nevirapine should be based on clinical experience and resistance testing (see section 5.1). (who.int)

Herein, we demonstrate apabetalone, the most clinical advanced BET inhibitor, downregulates expression of cell surface receptors involved in SARS-CoV-2 entry, including angiotensin-converting enzyme 2 (ACE2) and dipeptidyl-peptidase 4 (DPP4 or CD26) in SARS-CoV-2 permissive cells. (biorxiv.org)

The preliminary clinical results for a phase I b/II study investigating the PARP inhibitor Senaparib in combination with temozolomide (TMZ) for the treatment of advanced solid tumors have been presented as a poster at the 2022 ASCO Annual Meeting. (tmcnet.com)
Investigators conducted a pre-clinical trial in mice transplanted with kidney cancer from over 20 patients and showed that the HIF-2 inhibitor PT2399 controlled cancer in half of the tumors, according to a study published in the journal Nature . (eurekalert.org)
HIF-2 inhibitors work by suppressing the effects of HIF-2 which include downregulating an important protein called VEGF that promotes the formation of blood vessels needed for tumors to grow. (eurekalert.org)
Researchers surprisingly found a subset of tumors that do not respond to the drug, but were able to identify biomarkers that, once verified, would help determine which patients are more likely to benefit from HIF-2 therapies. (eurekalert.org)
These 2 theranostic approaches, as well as the therapy of osseous metastases of prostate cancer with 223 Ra ( 4 , 9 , 10 ), have unequivocally demonstrated that radionuclide therapy can be applied not only to thyroid cancer but also to other solid tumors. (snmjournals.org)
Although the present arsenal of Top1 inhibitors is effective in the treatment of solid tumors, their common camptothecin-based structure is plagued by physicochemical and pharmacological issues. (purdue.edu)
Gut stromal tumors and their clinical behavior. (medscape.com)

The aim of this review is to compare the clinical pharmacokinetics of available DPP-4 inhibitors (alogliptin, linagliptin, saxagliptin, sitagliptin and vildagliptin) for the purpose of identifying potential selection preferences according to individual patient variables and co-morbidities. (nih.gov)
Herein we report the effort beyond ACHN-975 to discover LpxC inhibitors optimized for enzyme potency, antibacterial activity, pharmacokinetics, and cardiovascular safety. (rcsb.org)

As sometimes happens in patients, mice on sunitinib were sickly and lost weight, whereas mice on the HIF-2 inhibitor gained weight while on the study," he said. (eurekalert.org)
A similar compound, sunitinib (Sutent), has been shown to be effective in patients with mutant GIST cells that are resistant to imatinib mesylate. (medscape.com)

Using a combination of targeted high-throughput screening and structure-based drug design, we have developed a series of aminopyrazole based FGFR inhibitors that covalently target a cysteine residue on the P-loop of the kinase. (rcsb.org)
Lenvatinib is oral multikinase inhibitor of VEGFR 1-3, FGFR 1-4, PDGFR-alpha, and RET and KIT proto-oncogenes. (esmo.org)

Unlike existing VEGF inhibitors, the HIF-2 inhibitor blocks VEGF only in the cancer and therefore does not cause cardiac toxicity or hypertension," Dr. Brugarolas explained. (eurekalert.org)
ACHN-975 (N-((S)-3-amino-1-(hydroxyamino)-3-methyl-1-oxobutan-2-yl)-4-(((1R,2R)-2-(hydroxymethyl)cyclopropyl)buta-1,3-diyn-1-yl)benzamide) was the first LpxC inhibitor to reach human clinical testing and was discovered to have a dose-limiting cardiovascular toxicity of transient hypotension without compensatory tachycardia. (rcsb.org)
Although many aspects of the biochemical toxicity of this compound are known, the cellular basis for the multiorgan dysfunction found at the clinical level is unclear. (medscape.com)
The toxicity data of protein kinase inhibitors in humans is also well established [5]. (who.int)
The toxicity of a particular arsenic compound depends in part on its solubility. (cdc.gov)
Other inorganic arsenic compounds may vary somewhat in relative toxicity, and organic arsenic compounds appear to be essentially nontoxic. (cdc.gov)

Lenvatinib, a multikinase inhibitor with activity against RET fusions, showed clinical benefit in patients with RET fusion-positive adenocarcinoma of the lung who demonstrated a disease control rate (DCR) of 76%,according to phase II study findings presented on 9 October at the ESMO 2016 Congress in Copenhagen, Denmark. (esmo.org)

In a previous report, Dr. Kevin Courtney, Assistant Professor of Internal Medicine and a coauthor of the current study, reported at the American Association of Clinical Oncology annual meeting that HIF-2 inhibitors were safe in patients and had activity even in heavily pretreated patients. (eurekalert.org)
Itraconazole, a common triazole anti-fungal drug in widespread clinical use, has evidence of clinical activity that is of interest in oncology. (ecancer.org)

They are irreversible competitive inhibitors of enzyme Acetyl Cholinesterase. (pediatriconcall.com)
[ 4 ] The enzyme has two isoforms: type 1 (found in the liver and skin) and 2 (found in reproductive tissues). (medscape.com)

SHANGHAI, China, Aug. 19, 2022 (GLOBE NEWSWIRE) -- IMPACT Therapeutics, a biopharmaceutical company dedicated to the discovery and development of targeted anti-cancer therapeutics based on synthetic lethality, announced today that the US Food and Drug Administration (FDA) has granted Orphan-Drug Designation (ODD) to our fixed-dose combination capsule of Senaparib (PARP inhibitor) and temozolomide (TMZ) for the treatment of adult patients with small cell lung cancer (SCLC). (tmcnet.com)
As no approved therapeutics exists to treat Covid-19, the disease associated to SARS-Cov-2, there is an urgent need to propose molecules that could quickly enter into clinics. (biorxiv.org)

Its pipeline product and programs include DNMT inhibitor, Oral DNMT inhibitor, dual IAP antagonist, oral murine double minute 2 (MDM2) antagonist and extracellular signal-related protein kinases inhibitor. (pharmaceutical-technology.com)

Today, α1-adrenoceptor blockers and 5α-reductase inhibitors are often combined to give a synergistic effect. (medscape.com)

Besides that, this review focuses on promising novel radiopharmaceuticals and describes their preclinical and clinical status. (snmjournals.org)

Concomitant administration of doxazosin tablets with a phosphodiesterase-5 (PDE-5) inhibitor can result in additive blood pressure lowering effects and symptomatic hypotension. (nih.gov)
Classes of medications include α1-adrenoceptor blockers, 5α-reductase inhibitors, and phosphodiesterase 5 inhibitors. (medscape.com)
Pharmacological BPH therapy protocols advocate the use of α-blockers (ABs) and 5α-reductase inhibitors (5ARI), individually or in combination, as well as phosphodiesterase-5 (PDE5) inhibitors, individually or concomitantly with ABs. (medscape.com)

The compound is an inhibitor of mammalian protein kinase and has been applied topically for the treatment of skin metastasis showing good local tolerability [5]. (who.int)
they are currently classified into three antigenic groups: group 1 and 2 include mammalian coronaviruses, and group 3 encompasses avian coronaviruses. (cdc.gov)

Constellation Pharmaceuticals has a pan-BRD inhibitor that is in a Phase 2 clinical trial in Ruxolitinib failures as monotherapy or in combination with Ruxolitinib. (moffitt.org)
ASTX-295 is under clinical development by Astex Pharmaceuticals and currently in Phase II for Solid Tumor. (pharmaceutical-technology.com)

The ORR was observed in 3 of 7 (42.9%) evaluable patients, including 2 confirmed PR who were still on treatment. (tmcnet.com)
The Phase 2b TAK-279 results demonstrate a strong overall clinical benefit and, importantly, a significant number of patients reached PASI 90 or 100, achieving near-total or total skin clearance," said April Armstrong, M.D., MPH, clinical investigator in the Phase 2b study and Associate Dean and Professor of Dermatology at the University of Southern California. (biospace.com)
RET fusions activate RET kinase and are seen in approximately 1% to 2% of patients with lung adenocarcinoma, prompting Vamsidhar Velcheti, Taussig Cancer Institute, Cleveland Clinic in Cleveland, USA and colleagues to investigate the efficacy of lenvatinib, a multikinase inhibitor with activity to RET, in an open label, phase II trial. (esmo.org)
15 (60%) patients received ≥2 prior lines of therapy, and 7 (28%) patients had received prior RET therapy. (esmo.org)
The investigators concluded that lenvatinib showed promising clinical activity in patients with RET-positive NSCLC, with most patients demonstrating tumour shrinkage and disease control. (esmo.org)
2 Clinical genetic data accumulated over the last 30 years indicate that a natural reduction in α-globin chain output by 25-50%, resulting from co-inherited α-thalassemia, ameliorates the disease phenotype in patients with β-thalassemia. (haematologica.org)
Lead compounds are superior to Ruxolitinib and Fedratinib at inhibiting the neoplastic cell growth of primary cells from MPN patients. (moffitt.org)
Management in symptomatic patients varies with the clinical syndrome. (medscape.com)
[ 2 ] In 1958, streptokinase was first used in patients with acute myocardial infarction (AMI), and this changed the focus of treatment. (medscape.com)
Clinical information and gene expression data of CRC patients were obtained from gene expression omnibus and the cancer genome atlas. (bvsalud.org)
Thus, efficacy is measured under expert supervision in a group of patients most likely to have a response to a drug, such as in a controlled clinical trial. (msdmanuals.com)
Advise clinicians that all hospitalized patients and all high-risk patients (either hospitalized or outpatient) with suspected influenza should be treated as soon as possible with a neuraminidase inhibitor antiviral. (cdc.gov)

Ruxolitinib-resistant cells however remained highly sensitive to our lead dual inhibitor compounds, potentially overcoming a major clinical bottleneck in the effectiveness of currently available JAK2 inhibitors. (moffitt.org)
The third effort was focused on making improvements to a promising class of indenoisoquinoline Top1 inhibitors, albeit one with a potentially serious toxicology risk. (purdue.edu)

A synergistic increase in cell killing occurs when myeloproliferative neoplasm primary cells are treated in combination with BRD4 and JAK2 inhibitors, or when AML cell lines are treated with inhibitors of BRD4 and FLT3. (moffitt.org)

Compared with the reference strain Wuhan/Hu-1/2019, the BA.1 and BA.2 variants have 36 and 31 amino acid substitutions in the S protein, respectively. (nature.com)
At the end of December 2019, scientists discovered the virus that came to be known as SARS-CoV-2-the pathogen behind the COVID-19 pandemic. (acs.org)
A novel coronavirus, named SARS-CoV-2, emerged in 2019 from Hubei region in China and rapidly spread worldwide. (biorxiv.org)
The coronavirus disease 2019 (COVID-19) pandemic, caused by the SARS-CoV-2 virus, has had a massive impact on human lives, health, and quality of life, challenging countries' healthcare systems and their economies worldwide. (elifesciences.org)
Severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) is responsible for the novel coronavirus disease of 2019 (COVID-19) 1 , a pandemic that has caused more than 2 million deaths worldwide, and continues to be a public health emergency 2 . (biorxiv.org)

Jamal GA. Neurological syndromes of organophosphorus compounds. (cdc.gov)

Hedgehog pathway inhibitor (IMP5471) has received IND approval from NMPA. (tmcnet.com)

When considered in total, data reviewed in this report suggest that the best overall balance between potency and the clinical pharmacokinetic characteristics of distribution, metabolism and elimination may be observed with linagliptin followed closely by vildagliptin, saxagliptin, sitagliptin and alogliptin. (nih.gov)

In 1997, UT Southwestern researchers Dr. Steven McKnight, Chairman of Biochemistry, and molecular geneticist Dr. David Russell, Vice Provost and Dean of Basic Research, led research discovering and describing the protein encoded by the EPAS1 gene, also known as HIF-2α, the main HIF-2 component. (eurekalert.org)
Virtual screening using molecular docking studies of the synthesized compounds was performed by (MOE), the molecular docking results indicate that, some synthesized compounds suitable inhibitor against (COX-2) with further modification. (scirp.org)

Aromatic ring substitution with 2,3-dimethoxy-8,9-methylenedioxy or a 3-nitro group was found to exert beneficial effects on antiproliferative and Top1 inhibitory activities. (purdue.edu)
The dimers, or bis(indenoisoquinolines), were decorated with the 2,3-dimethoxy-8,9-methylenedioxy aromatic ring substitution pattern on each monomer with the expectation of conferring high Top1 inhibitory activity. (purdue.edu)
Contrary to expectation, the Top1 inhibitory activities of the new compounds were weaker than those for aromatic ring-unsubstituted analogues. (purdue.edu)
Aspirin, glycoprotein (GP) IIb/IIIa inhibitors, and clopidogrel have an inhibitory effect on platelet activation and aggregation. (medscape.com)

In the second effort, thirty-two new indenoisoquinolines substituted with linear and cyclic carbohydrate-derived or carbohydrate-mimetic moieties were designed and synthesized as potential Top1 inhibitors. (purdue.edu)

An outbreak of atypical pneumonia, referred to as severe acute respiratory syndrome (SARS), was identified in the Guangdong Province of People's Republic of China at the end of 2002 and spread to other Asian countries and Canada ( 1 , 2 ) from February through March 2003. (cdc.gov)

Inhibitors of BRD4 are being explored clinically for the treatment of solid and hematologic cancers. (moffitt.org)

The compound is currently in a Phase III study for ovarian cancer, and Phase II studies for small cell lung cancer and other indications worldwide, including China. (tmcnet.com)
The lead clinical program, PARP inhibitor (Senaparib/ IMP4297), is in Phase II/III studies for ovarian cancer, small cell lung cancer and other indications worldwide, including China. (tmcnet.com)
Part of the SPORE grant, one of just two directly related to kidney cancer in the nation, is focused on further researching HIF-2 inhibitors. (eurekalert.org)
In the study in Nature, investigators show that HIF-2 inhibition was able to control metastatic kidney cancer even after 7 lines of prior therapy. (eurekalert.org)
The findings show that HIF-2 is a promising target to combat kidney cancer, said Dr. Brugarolas, senior author and a Virginia Murchison Linthicum Scholar in Medical Research at UT Southwestern. (eurekalert.org)
HIF-2 is believed to be the most important driver of kidney cancer. (eurekalert.org)
HIF-2 also appears significant in other types of cancer, including deadly brain cancers called glioblastomas and non-small cell lung cancer, the most common type of lung malignancy. (eurekalert.org)
In other recent news from Hanmi, the company announced on Tuesday that it had received approval for a Phase 2 clinical trial of HM61713, a targeted anti-cancer drug that selectively suppresses EGFR mutation. (drugdiscoverynews.com)
In this Phase 2 trial, Hanmi will evaluate HM61713's safety, speed and anti-cancer effects as a potential primary therapy for treating non-small cell lung cancer. (drugdiscoverynews.com)
Preclinical studies using BH3 mimetics have led to early phase studies of the BCL2 inhibitor venetoclax in breast cancer. (edu.au)
Ruxolotinib, Incyte's and Novartis' JAK1/JAK2 inhibitor, has already been approved for myelofibrosis, a rare bone cancer, as well as psoriasis, and rheumatoid arthritis, and had annual sales in 2018 of $1.4B. (moffitt.org)
These structures also illustrated the transporter cycle of ABCG2, the binding locations for inhibitors, and the link between cancer and the ABC transporter family. (proteopedia.org)
Given the evidence presented, a case is made that itraconazole warrants further clinical investigation as an anti- cancer agent. (ecancer.org)
A follow-up meeting on "Clinical Translation of Epigenetics in Cancer" was held in Charleston, SC, in January 2005. (aacrjournals.org)
As for GSK, it has been a very busy week for deals, having signed a £1.1 billion alliance with Denmark's Genmab for the latter's cancer and arthritis compound, HuMax-CD20, and a technology pact with Illumina. (pharmatimes.com)
The benzoxaborole compound impeded the growth of cancer cell lines derived from different lineages. (bvsalud.org)
Small bowel cancer: epidemiological and clinical characteristics from a population-based registry. (medscape.com)

This major clinical reference work comprises four volumes. (routledge.com)

Bromodomain-containing protein 4 (BRD4) is an epigenetic regulator that controls the expression of oncogenes such as c-Myc and Bcl-2. (moffitt.org)
The bromodomain and extraterminal (BET) family of epigenetic readers have been reported to modulate SARS-CoV-2 infection. (biorxiv.org)

from the basic mechanisms underlying the development of pain, to the various treatments that can be applied in different clinical situations. (routledge.com)
BTK plays a role in B cell development and maturation, and while the exact mechanism of action is unknown, BTK inhibitors have demonstrated anti-inflammatory and anti-tumor effects. (drugdiscoverynews.com)
Based on its overall profile, compound 26 (LPXC-516, (S)-N-(2-(hydroxyamino)-1-(3-methoxy-1,1-dioxidothietan-3-yl)-2-oxoethyl)-4-(6-hydroxyhexa-1,3-diyn-1-yl)benzamide) was chosen for further development. (rcsb.org)
1. DBT-BIRAC sponsored research project on "Development of Isothermal-PCR and CRISPR-Cas12 based rapid and portable coronavirus SARSCoV-2-COVID-19 detection kit"(50 lakhs, Co-PI)-(Ongoing). (wikieducator.org)
GlobalData's Likelihood of Approval analytics tool dynamically assesses and predicts how likely a drug will move to the next stage in clinical development (PTSR), as well as how likely the drug will be approved (LoA). (pharmaceutical-technology.com)
Our results suggest benzoxaboroles may represent a promising lead as CPSF3 inhibitors for clinical development. (bvsalud.org)

The spike (S) protein of SARS-CoV-2 mediates viral receptor binding and membrane fusion, both of which are essential for viral infection of host cells. (nature.com)
Complex relationships between rates of receptor binding and dissociation appear to strongly influence the durations of action of those DPP-4 inhibitors with comparatively shorter half-lives. (nih.gov)

Dipeptidyl peptidase-4 (DPP-4) inhibitors collectively comprise a presently unique form of disease management for persons with type 2 diabetes mellitus. (nih.gov)
We have an epidemic of type 2 diabetes that stresses limiting carbs. (thedr.com)

We show that 81.3-100% of individuals with high-viral-load SARS-CoV-2 nasopharyngeal-positive samples also test positive for PoST , suggesting this method is effective in identifying COVID-19 contagious individuals. (elifesciences.org)
Overall, we report that PoST is a new non-invasive, cost-effective, and easy-to-implement smartphone-based smart alternative for SARS-CoV-2 testing, which could help to contain COVID-19 outbreaks and identification of variants of concern in the years to come. (elifesciences.org)
The neuraminidase inhibitor (NAI) antiviral medications are most effective in treating influenza and reducing complications when treatment is started early. (cdc.gov)

INDIANAPOLIS- Eli Lilly and Co. and Hanmi Pharmaceutical Co. Ltd. , a global pharmaceutical company based in Seoul, have established an exclusive license and collaboration agreement to develop and commercialize Hanmi's oral Bruton's tyrosine kinase (BTK) inhibitor, HM71224, for the treatment of autoimmune diseases and other diseases. (drugdiscoverynews.com)
In the chapter devoted to older adults and mental health, the report emphasizes that older adults can benefit from recent advances in the treatment of psychiatric disorders and that these advances can prevent disability and promote the autonomy of older adults (2). (cdc.gov)
the guidelines for decontamination and medical treatment are applicable for exposure to arsenic and inorganic arsenic compounds, including arsenic trioxide. (cdc.gov)
Methodological bias in clinical studies, such as the subjective evaluation of the sexual side effect, makes it difficult to determine the ideal drug for treatment. (medscape.com)

Other DPP-4 inhibitors predominantly undergo renal excretion, with 60-85% of each dose eliminated as unchanged parent compound in the urine. (nih.gov)
ATR Inhibitor IMP9064 has received US IND Clearance from FDA and China IND application from NMPA and Phase I dose escalation is ongoing. (tmcnet.com)
Dose may be titrated at 1 to 2 week intervals, up to 8 mg once daily. (nih.gov)
The only detectable 14 C residues in the rat were from 14 C-methyl, representing 2-3 per cent of the dose. (inchem.org)
Neonatal dose: Under evaluation in Pediatric AIDS Clinical Trial Group protocol 332. (cdc.gov)

BIOLOGICAL DATA AND TOXICOLOGICAL EVALUATION Biochemical aspects Some knowledge has been obtained of the changes which the compound undergoes in plants. (inchem.org)

Should the compound successfully make it to market, Hanmi will also be eligible for tiered double-digit royalties. (drugdiscoverynews.com)
Also OncoEthix's OTX015 successfully completed Phase I clinical studies, and Merck acquired OncoEthix in December 2014 for $110M upfront and $265M in future milestones. (moffitt.org)
Furthermore, we successfully identified polymorphisms associated with SARS-CoV-2 Alpha, Beta, and Gamma variants, in SARS-CoV-2-positive PoST samples. (elifesciences.org)

Insecticides: organic phosphorus compounds and carbamates. (cdc.gov)
How has X-ray crystallography as a tool in organic chemistry changed over the last 2 decades? (rsc.org)
Arsenic compounds exist in a number of inorganic and organic forms. (cdc.gov)

We also observed a marked and significant reduction in the neutralizing activity of plasma from individuals who had recovered from COVID-19 and vaccine recipients against BA.2 compared to ancestral and Delta variant strains. (nature.com)
Here we characterized the functional activity of BA.2 variants in vivo. (nature.com)
The inhibitors show excellent activity against the wild-type and gatekeeper mutant versions of the enzymes. (rcsb.org)

In contrast to recent data with chimeric, recombinant SARS-CoV-2 strains expressing the spike proteins of BA.1 and BA.2 on an ancestral WK-521 backbone 4 , we observed similar infectivity and pathogenicity in mice and hamsters for BA.2 and BA.1, and less pathogenicity compared with early SARS-CoV-2 strains. (nature.com)
Preliminary data indicate that the BA.2 variant may be more transmissible than the BA.1 variant 5 , 6 . (nature.com)
Pregnant women are excluded from using this injectable, because as of now there is no clinical data for them. (theseoultimes.com)

Anatomy13

Organisms12

Chemicals and Drugs157

Analytical, Diagnostic and Therapeutic Techniques and Equipment36

Phenomena and Processes35

Disciplines and Occupations3

Technology, Industry, Agriculture2

Information Science4

Health Care2

Trials35

Small molecule3

Potent5

Therapeutic15

Kinase inhibitor2

Nucleoside reverse tr1

Anticancer3

Protease inhibitor3

Inhibit5

Histone4

Selective4

Vitro2

Orally3

Antiviral agents1

Targets5

Drugs7

Pesticides2

Resistance4

Downregulates1

Tumors7

Pharmacokinetics2

Sunitinib2

FGFR2

Toxicity6

20161

Oncology2

Enzyme2

Therapeutics2

Antagonist1

Synergistic effect1

Preclinical and clinical1

Phosphodiesterase3

Mammalian2

Pharmaceuticals2

Patients12

Potentially2

Combination1

20195

Syndromes1

Pathway1

Potency1

Molecular2

Inhibitory4

Designed and synthesized1

Respiratory1

Clinically1

Cancer17

Major clinical1

Bromodomain2

Development6

Receptor2

Type 2 diabet2

Effective3

Treatment4

Dose5

Undergoes1

Successfully3

Organic3

Activity3

Data3