• Hypoxia-Activated Prodrugs (HAPs) are prodrugs that target regions of tumor hypoxia within tumor cells. (wikipedia.org)
  • Different strategies to target hypoxic cancer cells and/or HIFs include hypoxia-activated prodrugs and inhibition of HIF dimerization, mRNA or protein expression, DNA binding capacity, and transcriptional activity. (lu.se)
  • Conclusion: A dibasic, self-activating prodrug (Compound 24) has been created which displays a much-increased lung tissue retention relative to the parent drug (Compound 1). (nottingham.ac.uk)
  • Here, we take a novel approach to produce a miR-127 prodrug (miR-127 PD ), which we demonstrate is processed to mature, functional miR-127-3p in TNBC tumor cells. (escholarship.org)
  • Now, a team of researchers at Kyoto University has developed a prodrug form of curcumin, TBP1901 , that has shown anti-tumor effects without toxicities. (polyphenols-site.com)
  • Several PET molecular imaging agents could be used for monitoring tumor responses to prodrug activation in gene therapy. (hindawi.com)
  • A common problem is that tumor heterogeneity prevents prodrugs from being adequately activated. (genengnews.com)
  • Werewolf Therapeutics develops tumor-activated immunotherapeutic prodrugs. (genengnews.com)
  • The prodrug strategy implementation in the last 20 y has led to a steady advancement in the biopharmaceutical, physicochemical and/or pharmacokinetic attributes of the pharmacologically active compounds. (ijpsonline.com)
  • We look forward to bringing EB-373 to clinical trials soon to assess the potential of this compound to elicit a more rapid onset of action, more controlled therapeutic effect, and reduced gastrointestinal side-effects compared to conventional psilocin prodrugs, such as psilocybin. (businesswire.com)
  • Therefore, In order to reduce the GCV dose required, we aim to compare the therapeutic efficacy of HSV1-sr39TK, an HSV1-TK mutant with increased GCV prodrug catalytic activity, with wildtype TK in C6 glioma cells. (hindawi.com)
  • This prodrug should constitute a versatile vehicle to explore new therapeutic targets and design more effective drugs in rare bowel diseases. (grstiftung.ch)
  • While more research is needed to determine the full extent of THCO's therapeutic potential, early studies suggest that this cannabinoid could be a powerful tool in the fight against various chronic diseases and conditions. (discovermagazine.com)
  • CBD is being studied for its potential therapeutic benefits, including reducing anxiety, relieving pain, and fighting cancer cells. (discovermagazine.com)
  • THCO is also being studied for its potential therapeutic benefits, including reducing inflammation and improving sleep quality. (discovermagazine.com)
  • My research interests are broadly based on the interface of synthetic organic chemistry and medicinal chemistry, and in particular on the drug discovery of bioactive molecules to probe biological systems or act as potential therapeutic agents in neuroscience, cancer/inflammation, infectious diseases, and other human conditions. (utmb.edu)
  • In this review, we discuss the changes in irradiated cancer cells and immune cells in the TME under different RT regimens and describe existing and potential molecules that could be targeted to improve the therapeutic effects of RT. (nature.com)
  • Elevating the therapeutic potential of cytokines. (ask-gene.com)
  • Therefore, therapeutic targeting of HIFs in cancer has the potential to improve treatment efficacy. (lu.se)
  • Therapeutic treatment with an oral prodrug of the remdesivir parental nucleoside is protective against SARS-CoV-2 pathogenesis in mice. (bvsalud.org)
  • In addition, the emergence of SARS-CoV-2 variants of concern, with their potential to escape neutralization by therapeutic monoclonal antibodies , emphasizes the need to develop second-generation oral antivirals targeting highly conserved viral proteins that can be rapidly deployed to outpatients . (bvsalud.org)
  • Here, we demonstrate the in vitro antiviral activity and in vivo therapeutic efficacy of GS-621763, an orally bioavailable prodrug of GS-441524, the parent nucleoside of remdesivir, which targets the highly conserved virus RNA-dependent RNA polymerase . (bvsalud.org)
  • The amino acid ester derivatives of 6-deoxypenciclovir, 11-20, were synthesized as potential prodrugs of penciclovir, and were evaluated for their oral penciclovir bioavailability in mice and rats. (ewha.ac.kr)
  • Valopicitabine (oral valine ester prodrug of 2′- C -methylcytidine). (cdc.gov)
  • Our goal is to create a best-in-class fumaric acid ester-based medicine for the potential treatment of relapsing-remitting MS and/or psoriasis. (news-medical.net)
  • The soon-to-issue patent, titled, "C4-Carbonothioate-substituted Tryptamine Derivatives and Methods of Using," contains composition of matter claims for a family of novel prodrug derivatives of psilocin, including EB-373, Enveric's lead product candidate. (businesswire.com)
  • Prodrugs are derivatives of drug molecules that are pharmacologically inactive but require either chemical or enzymatic transformation to release the active drug in vivo in order to exert a pharmacological effect. (ijpsonline.com)
  • The company's prodrugs are called Indukine molecules, and they are designed to unleash pro-inflammatory mechanisms on tumors while preventing unwanted side effects on nontarget tissue. (genengnews.com)
  • One of the company's IL-2 Indukine molecules, the WTX-124 prodrug, has shown promise in preclinical studies. (genengnews.com)
  • Werewolf Therapeutics also sees potential in one of its IL-12 Indukine molecules, the WTX-330 prodrug. (genengnews.com)
  • It outlines the discovery of compound 24 as a novel, dibasic, pH-sensitive, self-cleaving, muscarinic prodrug capable of withstanding enzymatic cleavage in order to liberate an active muscarinic receptor antagonist at a sustained rate over 24 hours. (nottingham.ac.uk)
  • Our study suggests that compound WRQ-2 is a potential gemcitabine prodrug and worth of further antitumor activity investigation. (go.jp)
  • It has the potential to become the first liver-targeted, orally administered drug for patients with HCC. (cision.com)
  • We previously described the synthesis of 1-O-octadecyl-2-O-benzyl-glycero-3-phospho-RVn (V2043), an orally bioavailable lipid prodrug of remdesivir nucleoside (RVn, GS-441524) with broad spectrum antiviral activity against viruses with pandemic potential. (cdc.gov)
  • Though several studies have been carried out on various prodrugs, surprisingly very few reviews on different carriers, which can be used for prodrug synthesis were published to date. (ijpsonline.com)
  • In this review different types of carriers, which can be used for prodrug synthesis are summarized. (ijpsonline.com)
  • The objective of this review is to provide the researchers with a compilation of which carriers would be suitable for prodrug synthesis and what would be their benefits. (ijpsonline.com)
  • In conclusion, our results demonstrate for the first time a potential regulatory mechanism modulating both the synthesis and degradation of heme, preventing the accumulation of toxic intermediates (ie. (unige.ch)
  • Included is the design and attempted synthesis of a series of prodrugs, which based on the results of chapter 1, would be interesting candidates for an in-vivo PK study to determine their duration of action relative to the parent drug candidates, and thus feasibility as sustained release delivery agents. (nottingham.ac.uk)
  • Before prescribing carbamazepine, the physician should be thoroughly familiar with the details of this prescribing information, particularly regarding use with other drugs, especially those which accentuate toxicity potential. (nih.gov)
  • By avoiding "cytokine sink" and peripheral toxicity, our SmartKine® platform significantly extends the pharmacokinetics of cytokines, powering next-generation prodrugs with improved safety profiles. (ask-gene.com)
  • Examples of both marketed and investigational prodrugs using several promoieties are discussed with their advantages and future prospects. (ijpsonline.com)
  • Results of a phase 2 study demonstrate potential Alzheimer's disease (AD)-modifying effects of an investigational oral anti-amyloid agent, represented by positive changes in plasma and imaging biomarkers of AD pathology. (medscape.com)
  • Vyvanse is a Schedule II substance in the US, which means that it has a high abuse potential, and its continued use can lead to severe psychological and physical dependence . (mentalhelp.net)
  • Because Vyvanse is a prodrug, it is not as susceptible to abuse as a pure amphetamine , but when recommended doses are exceeded, abuse is far more likely. (mentalhelp.net)
  • The newest stimulant medication approved by the FDA is Vyvanse ® , which is categorized as a "prodrug" because it is inactive until metabolized by the body. (greatschools.org)
  • These prodrugs subsequently undergo enzymatic or non-enzymatic cleavage to release the active drug moiety (figure 1) [ 12 , 13 ]. (ijpsonline.com)
  • Nucleic acids, such as antisense oligonucleotides (AONs) and small interfering RNAs (siRNAs) have enormous potential as therapeutics for life-threatening diseases because in principle, any problematic gene can be targeted with high efficacy and sequence-specificity. (grstiftung.ch)
  • We are also working on the discovery of DeltaFosB inhibitors, neurexin modulators, and FGF14/Nav1.6 channel complex protein-protein interaction inhibitors as CNS probes and potential therapeutics. (utmb.edu)
  • Tegafur, a prodrug of 5-fluorouracil (5-FU), is an oral fluorouracil antitumor drug used for the management of adenocarcinomas. (cun.es)
  • For example, a systemically administered prodrug could remain inactive until it reaches the TME, where it becomes activated and launches a powerful antitumor response. (genengnews.com)
  • This strong activity trade-off demonstrates that endogenous cellular metabolites hold considerable potential to shape evolutionary outcomes. (elifesciences.org)
  • Chapter 3: Develops further the prodrug system introduced in chapter 1, this time focusing on an intracellular PI3K δ target. (nottingham.ac.uk)
  • It has an efficacy similar to that of intravenous 5-FU, with potential advantages in terms of convenience and quality of life for the patient and cost-effectiveness as compared with intravenous chemotherapy. (cun.es)
  • As a side-reaction, NfsA has the potential to protect bacteria from an antibiotic called chloramphenicol, but it generally does this with such low efficacy that the effects are negligible. (elifesciences.org)
  • If zafirlukast is discontinued, hydrocodone plasma concentrations will decrease resulting in reduced efficacy of the opioid and potential withdrawal syndrome in a patient who has developed physical dependence to hydrocodone. (pdr.net)
  • ALZ-801 has shown potential for robust efficacy in the highest-risk Alzheimer's population - patients with two copies of the apolipoprotein ε4 allele (APOE4/4 homozygotes), and favorable safety with no increased risk of brain vasogenic edema, seen in trials with plaque-clearing antibodies. (biospace.com)
  • Phase 2 study results provide compelling evidence for potential efficacy of ALZ-801 in APOE4 carriers with Alzheimer's disease, who represent two thirds of Alzheimer's patients. (biospace.com)
  • These data also highlight the potential safety and efficacy advantages of ALZ-801 compared to plaque-clearing antibodies, while offering a simplified patient journey towards an effective treatment. (biospace.com)
  • Expands its intellectual property portfolio with composition of matter claims governing lead clinical candidate, EB-373, a psilocin prodrug being developed for the treatment of depression and anxiety disorders. (businesswire.com)
  • Among them, photodynamic therapy (PDT) has shown significant potential for the treatment and detection of cancer. (unige.ch)
  • Marinus will also host a scientific exhibit showcasing a series of posters highlighting the potential of ganaxolone in the treatment of refractory seizure disorders. (tmcnet.com)
  • In addition, Zevra is also advancing KP1077, a product candidate based on Zevra's prodrug of d-methylphenidate, serdexmethylphenidate ("SDX"), which is currently being evaluated in a Phase 2 trial for the treatment of idiopathic hypersomnia ("IH"), a rare sleep disorder. (yahoo.com)
  • The FDA has granted KP1077 orphan drug designation for the treatment of IH, and the U.S. Drug Enforcement Agency ("DEA") has classified SDX as a Schedule IV controlled substance based on evidence suggesting SDX has a lower potential for abuse when compared to d-MPH, a Schedule II controlled substance. (yahoo.com)
  • XenoPort completed three Phase 1 clinical trials of arbaclofen placarbil (AP) that are intended for inclusion in a potential 505(b)(2) new drug application (NDA) filing with the U.S. Food and Drug Administration (FDA) for the treatment of spasticity in patients with multiple sclerosis (MS) or spinal cord injury (SCI). (news-medical.net)
  • In particular, the successful Phase 1 bridging study provided information that we believe is critical to a potential 505(b)(2) NDA for AP for the treatment of spasticity in MS and SCI patients. (news-medical.net)
  • These data support the exploration of GS-441524 oral prodrugs for the treatment of COVID-19. (bvsalud.org)
  • These results support the continued development of V2043 and sn-2 glycerol modified RVn lipid prodrugs for the treatment of a broad range of RNA viruses for which there are limited therapies. (cdc.gov)
  • The company said that the FDA has lifted a full clinical hold on IDX184, a liver-targeted HCV nucleotide prodrug. (pmlive.com)
  • We have identified a suitable CPP-PNA structure for gene silencing and successfully synthesized the corresponding activatable CPP-PNA model prodrug for the local modulation of gene expression in the colon mucosa. (grstiftung.ch)
  • Of the prodrugs tested in mice and rats, 6-deoxypenciclovir O-l-valinate (13), O-l-isoleucinate (15), and O,O-di-glycinate (16) showed significantly higher urinary recovery of penciclovir compared with that of penciclovir, but those are somewhat lower than that of famciclovir. (ewha.ac.kr)
  • Evaluation of the method of increased lung tissue retention would then be explored using confocal microscopy to probe the lysosomal trapping potential of dibasic compounds. (nottingham.ac.uk)
  • The subsequent in-vivo pharmacokinetic studies demonstrate that when inhaled independently, over 99% of the active drug was eliminated from the lung tissue within 3 hours, but when delivered as a prodrug, sustained prodrug activation meant that the drug was present in the lung at a pharmaceutically relevant concentration for over 24 hours, with no detected exposure of the drug to blood plasma. (nottingham.ac.uk)
  • Chapter 4: Investigates how the dibasic moiety of the prodrug design affects the distribution of the prodrug in lung tissue. (nottingham.ac.uk)
  • Enveric has filed multiple composition of matter patent applications with the USPTO for psilocin prodrugs, including those comprising a crystalline molecular structure, and has submitted additional filings for companion Patent Cooperation Treaty and non-US national patent applications in an effort to obtain broad protections in target countries for its EVM201 and EVM301 Series of compounds. (businesswire.com)
  • Considering the range of chemical reactions involved in the biosynthetic pathways of Mtb , information related to the biotransformation of antitubercular compounds would provide opportunities for the development of new chemical tools to study successful TB infections while also highlighting potential areas for drug discovery, host-directed therapy, dose optimization and elucidation of mechanisms of action. (nature.com)
  • PF614 is a Trypsin Activated Abuse Protected (TAAP TM ) product designed as a delayed onset extended-release oxycodone prodrug. (accesswire.com)
  • Around 10 % of marketed medicines can be categorized as prodrugs currently, and also that during 2008, 33 % of approved small molecular weight drugs were prodrugs [ 5 - 7 ]. (ijpsonline.com)
  • We are led by a team of pioneering scientists focused on a shared goal: to make AskGene Pharma the global leader in cytokine prodrugs, providing safer and better medicines for saving patients' lives. (ask-gene.com)
  • HAPs may offer the potential, alone and in combination with conventional chemotherapy, of improving cancer therapy. (wikipedia.org)
  • Cite this: Oral Anti-Amyloid Shows Disease-Modifying Potential: Phase 2 Data - Medscape - Apr 28, 2023. (medscape.com)
  • SAN DIEGO, CA / ACCESSWIRE / April 3, 2023 / Ensysce Biosciences, Inc. ("Ensysce" or the "Company") (NASDAQ:ENSC), today announced positive results from a key study on the oral human abuse potential of PF614, a potential next generation pain medicine. (accesswire.com)
  • PF614 also had a significantly longer median time to reach peak levels for "Drug Liking" than oxycodone at all three dose levels, which is important for reducing abuse potential of opioid agents. (accesswire.com)
  • It is a prodrug that is metabolized by cytochrome P450 (CYP) enzymes CYP2D6 and CYP3A4 to its more potent opioid analgesic metabolites, particularly the O -demethylation product M1. (medscape.com)
  • Zevra expects several key milestones in 2023, including the planned resubmission of the New Drug Application ("NDA") for arimoclomol to the FDA as early as Q3 2023, an interim and final data readout for KP1077 in IH, and the potential achievement of one or more certain commercial sales milestones for our partnered asset, AZSTARYS ® , during FY 2023. (yahoo.com)
  • Enveric's lead program, the EVM201 Series, comprises next generation synthetic prodrugs of the active metabolite, psilocin. (businesswire.com)
  • Prodrug concept is justified because it enables the active drug to overcome the barrier that would impede it from reaching the site of action to exert the required pharmacological activity. (ijpsonline.com)
  • A bioprecursor prodrug is transformed chemically through hydration (for example, lactones such as some statins), reduction (for example, sulindac, platinum (IV) complexes) or oxidation (for example, dexpanthenol, nabumetone) or metabolically to the active agent [ 5 , 9 - 11 ]. (ijpsonline.com)
  • However, due to the potential endocrine disrupting properties of glucocorticoids, a tailored ERA for the active metabolite of beclometasone dipropionate (pro-drug), i.e. beclometasone-17-monopropionate (B17MP), had been performed. (janusinfo.se)
  • In contrast, codeine and tramadol are prodrugs: codeine is metabolized into morphine, and the active metabolite of tramadol is O -desmethyltramadol (M1). (medscape.com)
  • Properties and selection of carriers or promoeities is a very important parameter in successful prodrug design. (ijpsonline.com)
  • The aim of this project is to design a nucleic acid prodrug that is stable in the upper gastrointestinal tract, activated in the colon, and internalized in the colonic mucosa. (grstiftung.ch)
  • This chapter attempted to visualise the effect of incorporating a dibasic moiety into the prodrug design on the distribution and organelle sequestration. (nottingham.ac.uk)
  • The prodrug approach using various carriers has evolved as a significant tool in surmounting different obstacles in relation to drug formulation and targeting. (ijpsonline.com)
  • We are also requiring the drug manufacturers to conduct clinical trials to further evaluate the abuse potential of gabapentinoids, particularly in combination with opioids, with special attention being given to assessing the respiratory depressant effects," said Throckmorton. (medscape.com)
  • At the AACR event, one company reported that it is engineering interleukin-2 (IL-2) prodrugs that may be conditionally activated to minimize off-target effects. (genengnews.com)
  • ALZ-801 is an optimized prodrug of tramiprosate that has been shown to inhibit amyloid-beta 42 aggregation into toxic oligomers. (medscape.com)
  • It may last 8-10 hours and has been shown to have a lower abuse potential than traditional amphetamine. (greatschools.org)
  • The prodrug approach is rapidly becoming a crucial part in the stratagem of delivery of drugs. (ijpsonline.com)
  • The success of the prodrug approach can be measured by examining how many prodrugs are currently on the market. (ijpsonline.com)
  • An attractive cancer immunotherapy approach is the prodrug. (genengnews.com)
  • Pending the results from that trial, the Company plans to conduct a pivotal Phase 3 study in IH, with the potential to study an expanded indication in narcolepsy. (yahoo.com)
  • Prodrugs have better delivery properties that surpass the parent drug molecule [ 1 ]. (ijpsonline.com)
  • Biodegradable polymeric prodrugs for the delivery of antimalarial combination therapy. (sun.ac.za)
  • Chapter 2: Describes the use of prodrug systems as mechanisms for improving drug delivery. (nottingham.ac.uk)
  • Our Pacerone (Amiodarone HCl) Side Effects Drug Center provides a comprehensive view of available drug information on the potential side effects when taking this medication. (rxlist.com)
  • As with all cannabinoids, it's important to be aware of the potential risks and side effects before using THCO-containing products. (discovermagazine.com)
  • Carrier-linked prodrugs are for drugs with major drawbacks, which are linked to a nontoxic carrier or promoiety through covalent linkage to change or get rid of their undesirable physicochemical properties. (ijpsonline.com)
  • Among the most promising prodrugs employed nowadays, 5-ALA mediated PpIX gathers major recognition and promise. (unige.ch)
  • Beclomethasone dipropionate is a prodrug where the major metabolite is beclomethasone-17-monopropionate (B17MP). (janusinfo.se)
  • Unselected prodrug-converting activities were mostly unaffected, emphasising the importance of negative selection to effect enzyme specialisation, and offering an application for the evolved genes as dual-purpose selectable/counter-selectable markers. (elifesciences.org)
  • In response to these concerns, we are requiring updates to labeling of gabapentinoids to include new warnings of potential respiratory depressant effects. (medscape.com)
  • Here we compared the relative activity of V2043 with new RVn lipid prodrugs containing sn-1 alkyl ether or sn-2 glycerol modifications. (cdc.gov)
  • In this project, we propose to develop a prodrug platform of a polynucleotide conjugate that will be activated selectively in the colon lumen by bacterial enzymes which are present in the gut flora. (grstiftung.ch)