Astinova Blog
Working notes from the Astinova chemistry team — synthesis case studies, modality deep dives, and observations from real drug discovery programs.
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 →Why fluorinated amino acids, and why the (R)-series? Non-canonical amino acids are the building blocks of modern peptide drugs and designer biomaterials, and fluorine is one of the most powerful edits a chemist can make to one. Swapping a C–H…
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 →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…
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