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Estradiol dienanthate
go.drugbank.com/drugs/DB13955ApprovedVet approvedWithdrawnEstradiol is commonly produced with an ester side-chain as endogenous estradiol has very low oral bioavailability on its own (2-10%). … First-pass metabolism by the gut and the liver quickly degrades the estradiol molecule before it gets a chance to enter systemic circulation and exert its estrogenic effects [A12102].
Categories: Cytochrome P-450 CYP1A1 Substrates, Cytochrome P-450 SubstratesTasimelteon
go.drugbank.com/drugs/DB09071ApprovedInvestigationalBy activating melatonin receptors MT1 and MT2 in the suprachiasmatic nucleus of the brain, tasimelteon has been shown to improve sleep by resynchronizing the circadian rhythm through its "non-photic" mechanism … In blind individuals, a lack of light stimulation causes an extension of the 24-hour circadian cycle and can lead to progressively delayed sleep onset.
Categories: Cytochrome P-450 Substrates, Cytochrome P-450 CYP1A2 SubstratesE3 ubiquitin-protein ligase HUWE1
go.drugbank.com/bio_entities/BE0016469TargetHumansUbiquitinates MFN2 to negatively regulate mitochondrial fusion in response to decreased stearoylation of TFRC (PubMed:26214738). … Mediates HAPSTR1 degradation, but is also a required cofactor in the pathway by which HAPSTR1 governs stress signaling (PubMed:35776542).
Synonyms: Homologous to E6AP carboxyl terminus homologous protein 9Obeticholic acid
go.drugbank.com/drugs/DB05990ApprovedInvestigational[L34650] Obeticholic acid is currently being considered for FDA approval to treat fibrosis caused by non-alcoholic liver steatohepatitis (NASH). … hepatic decompensation) due to a risk of liver failure, in some cases requiring liver transplantation.
Synonyms: (3α,5β,6α,7α)-6-ethyl-3,7-dihydroxycholan-24-oic acidCategories: Cytochrome P-450 CYP1A2 Inhibitors, Cytochrome P-450 Enzyme InhibitorsRose bengal
go.drugbank.com/drugs/DB11182ApprovedInvestigationalThe clinical applications of rose bengal as injectable formulation under the name PV-10 in melanoma, breast cancer and skin conditions such as eczema and psoriasis are being investigated in clinical trials … Its disodium salt in ophthalmic solutions has been used as a diagnostic agent in suspected damage to conjunctival and corneal cells.
Voxelotor
go.drugbank.com/drugs/DB14975Approvedto 20 million others worldwide. … [L10403] It was developed by Global Blood Therapeutics, Inc.
Categories: Cytochrome P-450 Substrates, Cytochrome P-450 CYP2B6 SubstratesME-344
go.drugbank.com/drugs/DB13062InvestigationalME-344 has been used in trials studying the treatment of Solid Tumors.
Suplatast
go.drugbank.com/drugs/DB19138InvestigationalSuplatast is under investigation in clinical trial NCT05983471 (Efficacy and Safety of ME-015 (Suplatast Tosilate) in Cough Related to Idiopathic Pulmonary Fibrosis (COSMIC-IPF)).
Levoketoconazole
go.drugbank.com/drugs/DB05667Approved[A244083, A29319, L39573] Levoketoconazole was approved by the FDA on December 30, 2021, and is currently marketed under the registered trademark RECORLEV by Xeris Pharmaceuticals, Inc.[L39563] … [A244078, A244083] [Ketoconazole] has been used both on- and off-label to treat CS due to its ability to inhibit cortisol production.
Categories: Cytochrome P-450 Substrates, Cytochrome P-450 CYP1A2 InducersLG-100268
go.drugbank.com/drugs/DB01941ExperimentalLG-100268 is a retinoid X receptor (RXR) selective compound.