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Category: FDA approved small molecules

FDA approved small molecules· · 7 min read

synthesis of Gepotidacin (BLUJEPA) — Drug Intelligence Dossier

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…

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FDA approved small molecules· · 5 min read

Synthesis of Lenacapavir

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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FDA approved small molecules· · 5 min read

Synthesis of Remibrutinib (RHAPSIDO)

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…

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FDA approved small molecules· · 4 min read

Synthesis of Brensocatib (BRINSUPRI)

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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FDA approved small molecules· · 2 min read

Synthesis of Difamilast (ADQUEY)

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…

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