SSRIsSmall moleculeKinase inhibitorSSRIReuptake inhibitorsMonoaminePotent and selectiveCheckpoint inhibitorEfficacyInhibitionNSAIDsHighly potentTumorsTyrosineMAPKReceptorCyclooxygenaseCharacterizationFluvoxamine2018OutcomesEnzymeAllostericConcentrationsStructuralPoorlyTreatmentCompoundsEnzymesSelectivityPatientsSymptomsSuggestsResistanceRiskPhaseStudyFunctionalResponse
SSRIs14
- Selective Serotonin Reuptake Inhibitors (SSRIs) are a class of drugs that are typically employed as antidepressants in the treatment of major depressive disorders, anxiety disorders, and other psychological conditions. (wikipedia.org)
- The 2008 meta-analysis combined 35 clinical trials submitted to the Food and Drug Administration (FDA) before licensing of four newer antidepressants (including the SSRIs paroxetine and fluoxetine, the non-SSRI antidepressant nefazodone, and the serotonin and norepinephrine reuptake inhibitor (SNRI) venlafaxine). (wikipedia.org)
- Selective serotonin reuptake inhibitors ( SSRIs ), widely prescribed medications for the treatment of depression , obsessive-compulsive disorder , bulimia , anorexia nervosa , panic disorder , anxiety, and social phobia, have a high therapeutic to toxicity ratio. (medscape.com)
- SSRIs (Selective Serotonin Reuptake Inhibitors): What Are They? (healthline.com)
- Selective serotonin reuptake inhibitors (SSRIs) are a class of medications most often used to treat depression as well as a few other mental health conditions. (healthline.com)
- Because SSRIs have very little effect on other neurotransmitters in the brain like dopamine and norepinephrine, there are fewer reported side effects than tricyclic antidepressants (TCAs) and monoamine oxidase inhibitors (MAOIs) , which are other classes of antidepressants. (healthline.com)
- All of the SSRIs inhibit CYP2D6 but fluoxetine, norfluoxetine and paroxetine are particularly potent inhibitors. (biopsychiatry.com)
- We wanted to find out if medicines called selective serotonin re-uptake inhibitors (SSRIs), which are used mostly to treat depression, can help men that ejaculate faster than they want, to slow down. (cochrane.org)
- Selective serotonin re-uptake inhibitors (SSRIs), which are most commonly used as antidepressants are being used to treat this condition. (cochrane.org)
- Objective To establish whether an association exists between use of selective serotonin reuptake inhibitors (SSRIs) and suicide attempts. (bmj.com)
- Worldwide, selective serotonin reuptake inhibitors (SSRIs) are prescribed for the treatment of depression and an expanding list of additional conditions. (bmj.com)
- Purpose: Adverse effects of selective serotonin reuptake inhibitors (SSRIs) on sexual function have been an important area of research for many years. (soton.ac.uk)
- The purpose of this review is to evaluate the available literature regarding the use of selective serotonin reuptake inhibitors (SSRIs) and serotonin norepinephrine reuptake inhibitors (SNRIs) for the alleviation of VMS associated with menopause. (allenpress.com)
- We carried out a meta-analysis to evaluate the health effects of selective serotonin reuptake inhibitors (SSRIs) versus placebo or no antidepressants in patients with CHD and depression. (unife.it)
Small molecule4
- We are very pleased to advance CVN293, a selective small-molecule inhibitor of the novel target KCNK13 into Phase 1 clinical development," shared Craig Thompson, chief executive officer of Cerevance. (kron4.com)
- The identification of selective small-molecule inhibitors of histone demethylases would provide insight into the activity and cellular functions of these enzymes and also establish potential avenues for reversing pathologic epigenetic states. (aacrjournals.org)
- The FDA approval and commercial success of Velcade®, a small molecule proteasome inhibitor, has established the ubiquitin-proteasome system (UPS) as a valid target for anticancer treatment. (nih.gov)
- The potent and selective small molecule kinase inhibitor erlotinib (Erlo) was used in these experiments to block EGFR activation. (cdc.gov)
Kinase inhibitor2
- Our study examined the effect of a selective Rho kinase inhibitor, Y-27632, on corneal wound healing and potential stromal scarring after superficial keratectomy. (molvis.org)
- Objective: We aim to summarize recent studies related to the synthesis, mechanism of action, and clinical trials of the newly approved selective tyrosine kinase inhibitor entrectinib. (currentmedicinalchemistry.com)
SSRI4
- MEDLINE search (1966 to present) of OCD treatment with clomipramine or SSRI antidepressant medication using the key words obsessive-compulsive disorder, serotonin reuptake inhibitors, clomipramine, and pharmacology. (psychiatrist.com)
- The aim of this study was to comprehensively assess the role of genetic variation in FKBP5, identified by both Sanger and Next Generation DNA resequencing, as well as genome -wide single nucleotide polymorphisms ( SNPs ) associated with FKBP5 expression in the response to the selective serotonin reuptake inhibitor (SSRI) treatment of major depressive disorder . (bvsalud.org)
- Fluoxetine is an SSRI, selective serotonin reuptake inhibitor. (janusinfo.se)
- Depression in childhood and adolescence reuptake inhibitors (SSRI). (who.int)
Reuptake inhibitors5
- Venlafaxine (Effexor) and duloxetine (Cymbalta) are serotonin-norepinephrine reuptake inhibitors (SNRIs) that are also associated with serotonin toxicity, as is the tetracyclic drug mirtazapine (Remeron), an alpha-2 adrenergic heteroreceptor blocking agent that causes increased norepinephrine and serotonin release in addition to blocking serotonin receptors. (medscape.com)
- Selective serotonin reuptake inhibitors are very safe drugs, generally speaking," says Danny Carlat, MD, associate clinical professor of psychiatry at Tufts University School of Medicine. (healthline.com)
- The selective serotonin reuptake inhibitors fluoxetine, sertraline, fluvoxamine, and paroxetine have, in separate multicenter trials, demonstrated efficacy and tolerability in the treatment of OCD. (psychiatrist.com)
- While 2 recent meta-analyses support the superior efficacy of clomipramine over selective serotonin reuptake inhibitors in the treatment of OCD, 5 of 6 head-to-head comparisons of either fluoxetine or fluvoxamine versus clomipramine have found similar efficacy but a lower incidence of side effects with the selective serotonin reuptake inhibitor. (psychiatrist.com)
- The suggestion that selective serotonin reuptake inhibitors possess efficacy similar to that of clomipramine, but have a superior side effect profile, may have important implications for patients with OCD who require long-term treatment. (psychiatrist.com)
Monoamine4
- A New Potent and Selective Monoamine Oxidase-B Inhibitor with Extended Conjugation in a Chalcone Framework: 1-[4-(Morpholin-4-yl)phenyl]-5-phenylpenta-2,4-dien-1-one. (amrita.edu)
- The general blueprint for the design of monoamine oxidase-B (MAO-B) inhibitors has been based on two phenyl or heteronuclei linked via a spacer of appropriate length. (amrita.edu)
- The older types include tricyclic antidepressants (TCAs), tetracyclics, and monoamine oxidase inhibitors (MAOIs). (medlineplus.gov)
- The use of atomoxetine with monoamine oxidase inhibitors (MAOIs) is contraindicated. (medscape.com)
Potent and selective4
- CVN293 is an investigational, potent, and selective inhibitor of KCNK13, a novel target shown by NETSseq to be selectively expressed in brain microglia, a cell type that is central in neuroinflammation and has been implicated in many neurodegenerative diseases, including Amyotrophic Lateral Sclerosis, Alzheimer's disease and severe age-related macular degeneration. (kron4.com)
- 3-[3-Amino-4-(indan-2-yloxy)-5-(1-methyl-1 H -indazol-5-yl)-phenyl]-propionic acid (AK106-001616) is a novel, potent, and selective inhibitor of the cytosolic phospholipase A 2 (cPLA 2 ) enzyme. (aspetjournals.org)
- These compounds are the most potent and selective DUB inhibitors reported to date. (nih.gov)
- Represents the most potent and selective DUB inhibitor reported to date. (nih.gov)
Checkpoint inhibitor2
- The BGBIL006 trial is a randomised Phase 1b /2 investigator sponsored clinical study of bemcentinib (BGB324) in combination with either the MAPK inhibitors MEKINIST® (trametinib) plus TAFINLAR® (dabrafenib) or the immune checkpoint inhibitor KEYTRUDA® (pembrolizumab) in patients with advanced melanoma. (prnewswire.co.uk)
- Objective responders include patients with tumors harboring BRAF V600E that had progressed on prior BRAF/MEK inhibitors with or without checkpoint inhibitor treatment, BRAF Class II mutation, BRAF fusion, NRAS and KRAS mutations. (financialcontent.com)
Efficacy1
- These results suggest the inhibitors may also improve the efficacy and potency of other commonly prescribed chemotherapeutic agents that are known to induce DNA damage. (nih.gov)
Inhibition4
- Selective cyclooxygenase-1 (COX-1) inhibition has got into the spotlight with the discovery of COX-1 upregulation in various cancers and the cardioprotective role of COX-1 in control of thrombocyte aggregation. (cas.cz)
- PHI1 exhibits discrete cellular selectivity for BRAF dimers, with enhanced inhibition of the second protomer when the first protomer is occupied, comprising a novel class of dimer selective inhibitors. (nature.com)
- Promising alternative to proteasome inhibition offering the potential of more selective and less toxic therapeutic agents. (nih.gov)
- Hg(II), cytochalasin B (cytB) and forskolin, inhibitors of glucose transportation via GLUTs, decreased glucose transportation but had small inhibition on CH3As(OH)2 transportation. (edrc2013.org)
NSAIDs2
- This assertion is borne out by recent clinical studies showing that the COX-2 inhibitors rofecoxib and celecoxib procedure qualitative changes in urinary prostaglandin excretion, glomerular filtration rate, sodium retention, and their consequences similar to nonselective NSAIDs. (nih.gov)
- It, therefore, seems unlikely that these COX-2 inhibitors (and perhaps their successors) will offer renal safety benefits over nonselective NSAID therapies, and, at this juncture, it is reasonable to assume that all NSAIDs, including COX-2-selective inhibitors, share a similar risk for adverse renal effects. (nih.gov)
Highly potent1
- Background: Entrectinib is a highly potent ATP-competitive and selective inhibitor of tyrosine kinases - Trk A B C, ALK, and ROS1. (currentmedicinalchemistry.com)
Tumors3
- SSE: 688235), and SpringWorks Therapeutics, Inc. (NASDAQ: SWTX), today announced that they will present updated clinical data from the Phase 1a/1b study of BGB-3245, an investigational, selective RAF dimer inhibitor, in adult patients with advanced or refractory solid tumors harboring MAPK pathway aberrations. (financialcontent.com)
- These data support the ongoing investigation of BGB-3245 in defined cohorts, including BRAF V600 tumors that have progressed after prior BRAF and/or MEK inhibitor treatment, solid tumors with BRAF class II mutations and BRAF fusions, and NRAS mutant melanoma," said Alison M. Schram, M.D., Assistant Attending Physician at Memorial Sloan Kettering Cancer Center in New York. (financialcontent.com)
- This work shows that Ponatinib and BRAF dimer selective inhibitors will be useful in treating BRAF-dependent tumors. (nature.com)
Tyrosine3
- OSAKA, JAPAN & CAMBRIDGE, MASS.--( Business Wire / Korea Newswire ) September 12, 2023 -- Takeda ( TSE:4502/NYSE:TAK ) today announced positive topline results from its randomized, double-blind, placebo-controlled, multiple-dose Phase 2b trial evaluating TAK-279, an investigational oral allosteric tyrosine kinase 2 (TYK2) inhibitor with next generation selectivity, in people with active psoriatic arthritis. (koreanewswire.co.kr)
- TAK-279 is a highly selective, oral allosteric tyrosine kinase 2 (TYK2) inhibitor in late-stage development,[6] with approximately 1.3 million-fold greater selectivity for TYK2 as compared with JAK1. (koreanewswire.co.kr)
- Takeda ( TSE:4502/NYSE:TAK ) today announced positive topline results from its randomized, double-blind, placebo-controlled, multiple-dose Phase 2b trial evaluating TAK-279, an investigational oral allosteric tyrosine kinase 2 (TYK2) inhibitor with next generation selectivity, in people with active psoriatic arthritis. (cbinews.com)
MAPK2
- The promising data we are sharing at AACR demonstrate the value of our next-generation RAF dimer inhibitor, BGB-3245, as a monotherapy in patients with MAPK pathway-altered cancers, especially its potential to address key primary and resistance gene alterations that are currently unaddressed by approved therapies," said Lusong Luo, Ph.D., Acting CEO of MapKure and Senior Vice President, External Innovation at BeiGene. (financialcontent.com)
- Results demonstrated that BGB-3245 had a manageable safety profile, with adverse event findings consistent with other MAPK pathway inhibitors. (financialcontent.com)
Receptor3
- METHODS: To study the complexity of the mechanisms involved in the resistance to the selective estrogen receptor degrader (SERD) fulvestrant, we performed comprehensive biomarker analyses using several in vitro models that recapitulate the heterogeneity of developed resistance. (lu.se)
- CONCLUSIONS: These data highlight the complexity of estrogen receptor positive breast cancer and suggest that the development of diverse resistance mechanisms dictate levels of ER independence and potentially cross-resistance to CDK inhibitors. (lu.se)
- Substitution of medications that may cause oral burning (If an angiotensin-converting enzyme [ACE] inhibitor, angiotensin 2 receptor blocker [ARB], or antiretroviral is suspected, trying another medication in the same class is reasonable. (medscape.com)
Cyclooxygenase2
- Unlike traditional nonsteroidal anti-inflammatory drugs and selective cyclooxygenase-2 inhibitors, AK106-001616 reduced prostaglandin E 2 (PGE 2 ) and leukotriene B 4 (LTB 4 ) production by stimulated cells. (aspetjournals.org)
- The global " non-steroidal anti-inflammatory drugs " market is set to gain momentum from the ever-increasing research activities by several prominent pharmaceutical companies on selective cyclooxygenase-2 inhibitors as they are still a grey area for these companies. (medgadget.com)
Characterization1
- The identification and characterization of a selective H3K27me3 inhibitor thus provides insight into the structural determinants and cellular roles of demethylase activity, which may benefit cancer epigenetic drug discovery efforts. (aacrjournals.org)
Fluvoxamine1
- Although not metabolized by CYP2C19, fluvoxamine is still a potent inhibitor of the enzyme. (biopsychiatry.com)
20181
- Bergen, NORWAY , Oct. 9, 2018 /PRNewswire/ -- BerGenBio ASA (OSE:BGBIO) announces that the company and its collaborators will present interim clinical and biomarker data from its Phase II clinical programme with bemcentinib (BGB324), a first-in-class highly selective oral AXL inhibitor at the ESMO 2018 Congress in Munich (19 - 23 October 2018). (prnewswire.co.uk)
Outcomes2
- These Phase 2b results highlight the potential of TAK-279, a highly selective, oral TYK2 inhibitor, to improve clinical outcomes for people living with psoriatic arthritis," said Andy Plump, President R&D, Takeda. (koreanewswire.co.kr)
- FKBP5 genetic variation: association with selective serotonin reuptake inhibitor treatment outcomes in major depressive disorder. (bvsalud.org)
Enzyme1
- Available for licensing are inhibitors that target the USP1/ UAF1 deubiquitinating enzyme (DUB) complex. (nih.gov)
Allosteric1
- Using these structural insights, we developed PHI1, a BRAF inhibitor that fully uncovers the allosteric site. (nature.com)
Concentrations1
- Based on these data and expected tissue concentrations of inhibitors, we predict that a p.o. administered curcuminoid/piperine combination is most likely to inhibit CYP3A, CYP2C9, UGT, and SULT metabolism within the intestinal mucosa. (aspetjournals.org)
Structural1
- These structural insights provide a framework for future development of histone demethylase inhibitors. (aacrjournals.org)
Poorly2
- Yet, COX-1-selective inhibitors are poorly explored. (cas.cz)
- FDA-approved RAF inhibitors poorly inhibit BRAF dimers, which leads to tumor resistance. (nature.com)
Treatment1
- given the association between cardiovascular risk and exposure to COX-II inhibitors, doctors are advised to use the lowest effective dose for the shortest possible duration of treatment. (gpnotebook.com)
Compounds2
- Kruidenier and colleagues solved the crystal structure of the JMJD3 catalytic domain in complex with an H3K27me3 peptide and used the insights into interactions required for substrate specificity and recognition to guide the optimization of weak inhibitors discovered in a screen of 2 million compounds. (aacrjournals.org)
- Of the prepared compounds, 11 exhibited interesting COX-1 selectivity, with 8 compounds being totally COX-1-selective. (cas.cz)
Enzymes1
- 2005 ). cAMP and cGMP are hydrolyzed by phosphodiesterase (PDE) enzymes, and inhibitors of PDEs (PDE-Is) produce cognition-enhancing effects in animal models of cognition. (springer.com)
Selectivity1
- Three classes of inhibitors with this scaffold were synthesized and tested for their nNOS activity and eNOS selectivity. (rsc.org)
Patients7
- Fedratinib, an oral, selective Janus-kinase 2 (JAK2) inhibitor, was investigated in the randomized, placebo-controlled, phase III JAKARTA study in adult patients with intermediate- or high-risk JAK-inhibitor-naïve MF. (iasp-pain.org)
- Fedratinib provided clinically meaningful improvements in MF symptoms and overall HRQoL versus placebo in patients with JAK-inhibitor-naïve MF. (iasp-pain.org)
- The study met its primary endpoint with a greater proportion of patients treated once-daily with TAK-279 achieving at least a 20 percent improvement in signs and symptoms of disease (American College of Rheumatology 20 response) at week 12 compared to placebo, supporting its potential as a highly selective oral option for patients with psoriatic arthritis. (koreanewswire.co.kr)
- for all patients the balance of GI and cardiovascular risk should be considered before prescribing a COX-2 inhibitor, particularly for those with risk factors for heart disease (such as hypertension, hyperlipidaemia, diabetes and smoking, as well as for patients with peripheral arterial disease) and those taking low dose aspirin, for whom GI benefit has not been clearly demonstrated. (gpnotebook.com)
- COX-II inhibitors must not be used in patients with established ischaemic heart disease and/or cerebrovascular disease, and also in patients with peripheral arterial disease. (gpnotebook.com)
- caution should be exercised when prescribing COX-II inhibitors to patients with risk factors for heart disease, such as hypertension, hyperlipidaemia, diabetes and smoking. (gpnotebook.com)
- However, drug resistance to these inhibitors is developed resulting in only short-term improvement of patients' survival 15 . (nature.com)
Symptoms1
- Patient-reported Effects of Fedratinib, an Oral, Selective Inhibitor of Janus Kinase 2, on Myelofibrosis-related Symptoms and Health-related Quality of Life in the Randomized, Placebo-controlled, Phase III JAKARTA Trial. (iasp-pain.org)
Suggests1
- evidence suggests that selective COX-2 inhibitors, as a class, may cause an increased risk of thrombotic events (e.g. (gpnotebook.com)
Resistance2
- During the past year we have optimized the antiviral activity of two distinct series of GAK inhibitors and a series of AAK1 inhibitors, all with excellent broad- spectrum antiviral activity (DENV, CHIKV and EBOV and SARS-CoV-2), including in human primary cells, with a high barrier to resistance. (dtic.mil)
- However, proteasome inhibitors in general suffer from a narrow therapeutic index and acquired resistance. (nih.gov)
Risk1
- Do selective cyclo-oxygenase-2 inhibitors and traditional non-steroidal anti-inflammatory drugs increase the risk of atherothrombosis? (bmj.com)
Phase1
- The company's proprietary lead candidate, bemcentinib, is a potentially first-in-class selective AXL inhibitor in a broad phase II clinical development programme. (prnewswire.co.uk)
Study1
- The present study investigates the effect of the PDE4 inhibitor rolipram and the PDE5 inhibitor sildenafil on object retrieval performance. (springer.com)
Functional1
- A number of highly selective and potent factor Xa (FXa) and FIXa inhibitors were identified by simple switch of functional groups with conformational changes toward the S2-S4 sites. (rcsb.org)
Response1
- A selective jumonji H3K27 demethylase inhibitor modulates the proinflammatory macrophage response. (aacrjournals.org)