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合計43件の記事
Lipfendra Approval Puts Oral Macrocyclic Peptide Process Design in Focus
FDA announced on July 16, 2026 that Lipfendra (enlicitide) was approved to be used with diet and exercise to reduce LDL-C in adults with high cholesterol or heterozygous familial hypercholesterolemia. FDA also states that Lipfendra is a tablet taken by mouth once daily and is the first oral therapy that blocks PCSK9.
LUNA18 Shows Why N-Alkyl-Rich Cyclic Peptides Need Route-Specific Process Design
The key correction is that the ACS Organic Process Research & Development paper describes LUNA18 (paluratide) through a liquid-phase peptide synthesis process, not a simple SPPS plus three-fragment route. The paper’s abstract says the authors departed from conventional solid-phase peptide synthesis and developed an LPPS process for an N-alkyl-rich cyclic undecapeptide KRAS inhibitor.
Reported Inclisiran GalNAc-siRNA Architecture: Conjugation and DMPK
The reported inclisiran architecture illustrates why an siRNA conjugate cannot be reduced to a sequence plus a targeting ligand. Descriptions of that architecture place a triantennary N-acetylgalactosamine (GalNAc) unit at the sense-strand terminus, combine 2'-fluoro and 2'-O-methyl ribose substitutions with terminal phosphorothioate linkages, and rely on the antisense strand for RNA-induced silencing complex (RISC) loading. Each element addresses a different constraint: cell uptake, nuclease exposure, strand handling, or intracellular recognition.
Reported Iron-Core CO-Releasing Module Broadens ADC Payload Design
Crossref metadata verifies the primary paper's title, authorship, journal, DOI, and publication record. The detailed construct is reported as combining an Fe(CO)3 CO-releasing molecule, a Val-Cit-PABC trigger, and thiol conjugation to trastuzumab after interchain disulfide reduction.
A Preprint Maps siRNA 5′-Phosphate Chemistry for AGO2 Anchoring
The siRNA guide-strand 5′-phosphate is a recognition element for engagement with the AGO2 MID domain. The preprint examines a different way to modify that terminus: installing an organic substituent on a nonbridging phosphate oxygen while retaining a phosphate-centered anchoring group.
Reported PBD Dimer Chemistry for ADC Linker–Payload Design
Pyrrolobenzodiazepine (PBD) dimers join two PBD units to create a bifunctional DNA-reactive scaffold. For ADC development, the useful question is not which free payload appears most potent in an isolated assay. It is how electrophile state, linker architecture, hydrophilicity, conjugation level, release behavior, and analytical control work together in the complete linker–payload and conjugate.