Astinova Blog
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 →How a single small molecule can staple two proteins together and send one of them to the cellular shredder — the mechanism, the medicinal-chemistry logic, and a worked synthesis of the archetypal drug. 1. Why “glue” is the…
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…
Read article →Compiled: 2026-06-17 · Trigger event: FDA approval, 2025-09-30 Innovator: Novartis Pharmaceuticals Corporation Status: Approved NME INN: remibrutinibBrand (US): RHAPSIDOCAS: 1787294-07-8ChEMBL: CHEMBL4483575MW: 507.5 g/molNDA #: NDA 218436Approval: 2025-09-30 Mechanism: Remibrutinib is an oral, small-molecule covalent (irreversible) inhibitor of Bruton’s tyrosine kinase (BTK), engaging the catalytic Cys481 via its acrylamide warhead and binding an inactive…
Read article →Compiled: 2026-06-16 · Trigger event: FDA approval, 2025-08-12 Innovator: Insmed Incorporated (originator AstraZeneca; AZD7986, worldwide-licensed to Insmed Oct 2016 as INS1007) Status: Approved NME INN: brensocatibBrand (US): BRINSUPRICAS: 1802148-05-5ChEMBL: CHEMBL3900409MW: 420.5 g/molNDA #: NDA 217673Approval: 2025-08-12 Mechanism: Brensocatib is a competitive, reversible (reversible-covalent, via a nitrile warhead engaging the catalytic Cys) inhibitor of…
Read article →Patent / Application Type Assignee Filed Expiry (~) WO 2007/058338 A1 (US 7,919,617 B2; EP 1,953,148 B1; JP 4,975,757 B2) Composition of matter (originator) Otsuka Pharmaceutical Co., Ltd. 2006-11-16 (priority 2005-11-15, JP 2005-330289) ~Nov 2026 nominal (US 7,919,617…
Read article →Patent Landscape & Exclusivity 2.1 Key patent filings Synthesis Route of the Originator Convergent synthesis disclosed in WO 2014/135561 (Roche). Eastern fragment: 1-methyl-6-bromo-3,4-dihydroquinolin-2(1H)-one (INT-2) → pinacolboronate (INT-3, via Pd/B2pin2 Miyaura). Western fragment: (R)-8-aminotetrahydroisoquinoline scaffold, Boc-protected (INT-5), 4-bromide for…
Read article →In the conventional ADC narrative, the antibody picks the cell, the payload kills it, and the linker just holds them together until they get there. The picture is wrong in roughly the same way that calling a fuel…
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