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Mechanism: Lirafugratinib (RLY-4008) is a highly selective, IRREVERSIBLE (covalent) small-molecule inhibitor of fibroblast growth factor receptor 2 (FGFR2). A methacrylamide (2-methylprop-2-enamide) Michael-acceptor warhead covalently engages Cys491 at the tip of the FGFR2 phosphate-binding (P)-loop (homologous Cys488 in FGFR1). Selectivity…
Read article →Mechanism: Iberdomide is a potent, orally available cereblon (CRBN) E3 ligase modulator (CELMoD). It binds CRBN — the substrate receptor of the CRL4^CRBN E3 ubiquitin ligase — and reshapes the substrate-recruitment surface to drive ubiquitination and proteasomal degradation of…
Read article →Mechanism: Brepocitinib is an oral, Type I (ATP-competitive) inhibitor that reversibly binds the catalytic JH1 kinase domain of BOTH tyrosine kinase 2 (TYK2; ChEMBL CHEMBL3553) and Janus kinase 1 (JAK1; CHEMBL2835), with relative JAK2/JAK3 sparing (enzymatic IC50 ~TYK2 23…
Read article →Mechanism: Daraxonrasib (RMC-6236) is an oral, noncovalent, beyond-Rule-of-5 macrocyclic ‘tri-complex’ (molecular-glue) inhibitor of RAS. It first binds the intracellular chaperone cyclophilin A (CypA); the drug–CypA binary complex then presents a neomorphic composite surface that engages the active, GTP-bound (‘ON’)…
Read article →Compiled: 2026-08-14 · Trigger event: FDA approval, 2025-03-25 Innovator: GlaxoSmithKline LLC (US NDA holder; composition-of-matter patents held by Glaxo Group Limited). Developed with US government biodefense co-funding (BARDA OTA HHSO100201300011C; DoD/DTRA HDTRA1-07-9-0002). Status: Approved NME Mechanism: Gepotidacin is a first-in-class, bactericidal TRIAZAACENAPHTHYLENE antibacterial that inhibits bacterial…
Read article →The switch that runs your day Deep in the hypothalamus, a small population of neurons produces two neuropeptides — orexin-A and orexin-B (also called hypocretin-1 and -2). They are the master “stay awake” signal, acting on two G-protein-coupled receptors, OX1R and OX2R. Of…
Read article →Mechanism: Zidesamtinib is a small-molecule inhibitor of the tyrosine kinase ROS1, including ROS1 resistance mutations. In biochemical assays (PI §12.1) it inhibits ROS1 (IC50 = 0.7 nM) with much weaker activity against the tropomyosin receptor kinases — TRKB (IC50…
Read article →Bristol Myers Squibb’s oral CELMoD is the first cereblon modulator designed from the ground up for fast, deep protein degradation — and its positive Phase 3 SUCCESSOR-2 readout signals a new standard for relapsed/refractory multiple myeloma. 1. Why…
Read article →Field Value Target name Bromodomain-containing protein 4 (BRD4); BET family member (UniProt O60885) Gene BRD4 — chromosome 19p13.12; NCBI Gene 23476 Class Epigenetic ‘reader’. BET (Bromodomain & Extra-Terminal) family — two tandem bromodomains (BD1, BD2) plus an ET…
Read article →Lenacapavir (YEZTUGO (PrEP) and SUNLENCA (HIV-1 treatment)) — Drug Intelligence Dossier Compiled: 2026-06-17 · Trigger event: FDA approval, 2025-06-18 Innovator: Gilead Sciences, Inc. (development code GS-6207) Status: Approved NME INN: lenacapavirBrand (US): YEZTUGO (PrEP) and SUNLENCA (HIV-1 treatment)CAS: 2189684-44-2ChEMBL: —MW: 968.3 g/molNDA #: NDA 220020 / 220018 (YEZTUGO, PrEP); original NME…
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