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Pirtobrutinib
go.drugbank.com/drugs/DB17472ApprovedInvestigationalPirtobrutinib is a small molecule and a highly selective non-covalent inhibitor of Bruton’s tyrosine kinase (BTK). Its high selectivity has been associated with lower discontinuation rates due to adverse events and a lower incidence of a...
Categories: P-glycoprotein inhibitors, P-glycoprotein substratesVimseltinib
go.drugbank.com/drugs/DB17520ApprovedInvestigationalVimseltinib is a small molecule kinase inhibitor targeting colony-stimulating factor 1 receptor (CSF1R). It is highly selective, with a >500-fold selectivity for CSF1R over its nearest off-target kinase. It is intended to provide a sa...
Categories: P-glycoprotein inhibitors, P-glycoprotein substratesRilzabrutinib
go.drugbank.com/drugs/DB17709ApprovedInvestigationalRilzabrutinib is an oral, reversible, covalent inhibitor of Bruton's tyrosine kinase that was approved by the FDA on August 29, 2025, for the treatment of persistent and chronic immune thrombocytopenia (ITP). ITP is an autoimmune disorde...
Categories: P-glycoprotein inhibitors, P-glycoprotein substratesSebetralstat
go.drugbank.com/drugs/DB18305ApprovedInvestigationalHereditary angioedema (HAE) is a rare genetic disease that causes sudden, painful swelling episodes in various body locations that can be life-threatening, particularly when affecting the throat . Sebetralstat is the first and only oral ...
Categories: P-glycoprotein substrates, Cytochrome P-450 SubstratesAficamten
go.drugbank.com/drugs/DB18490ApprovedInvestigationalAficamten is a cardiac myosin inhibitor. Approved by the FDA on December 19, 2025, aficamten is indicated for the treatment of adults with symptomatic obstructive hypertrophic cardiomyopathy (oHCM) to improve functional capacity and symp...
Categories: Cytochrome P-450 Substrates, Cytochrome P-450 CYP2C19 SubstratesZongertinib
go.drugbank.com/drugs/DB18762ApprovedInvestigationalZongertinib is a selective, irreversible tyrosine kinase inhibitor that targets human epidermal growth factor receptor 2 (HER2). It covalently binds to the HER2 receptor, including exon 20 insertions, and inhibits downstream signaling pa...
Categories: Cytochrome P-450 Substrates, Cytochrome P-450 CYP3A SubstratesDeuruxolitinib
go.drugbank.com/drugs/DB18847ApprovedInvestigationalDeuruxolitinib is a deuterated form of ruxolitinib that selectively inhibits Janus kinases (JAK) JAK1 and JAK2. Deuteration allows the drug to circumvent extensive oxidative metabolism around the cyclopentyl ring, which increases the dur...
Categories: P-glycoprotein substrates, Cytochrome P-450 SubstratesSunvozertinib
go.drugbank.com/drugs/DB18925InvestigationalSunvozertinib is an irreversible and selective epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor. EGFR is a transmembrane protein with cytoplasmic kinase activity commonly expressed by non-small cell lung carcinomas (NSCL...
Categories: P-glycoprotein inhibitors, Cytochrome P-450 SubstratesSuzetrigine
go.drugbank.com/drugs/DB18927ApprovedInvestigationalSuzetrigine is a NaV1.8 voltage-gated sodium channel blocker with analgesic properties NaV1.8 is abundantly expressed in peripheral sensory nerves to play a role in pain signal transmission, making it a desirable therapeutic target for t...
Categories: P-glycoprotein substrates, Cytochrome P-450 CYP2B6 InducersOrforglipron
go.drugbank.com/drugs/DB18964ApprovedInvestigationalOrforglipron is a first-in-class oral, non-peptide glucagon-like peptide-1 (GLP-1) receptor agonist. Developed to circumvent the adherence barriers and strict administration requirements of peptide-based GLP-1 therapies, its small-molecu...
Categories: Cytochrome P-450 Substrates, P-glycoprotein substrates