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Revisiting ritonavir’s polymorph landscape, the authors examined whether crystal structure prediction could have flagged the risk posed by the less soluble Form 2. They also solved the previously unresolved Form 4 structure using 3D electron diffraction, modeling, and powder X-ray diffraction, finding disorder and thermodynamic instability. The retrospective analysis informs risk assessment rather than guaranteeing future polymorph prediction.
Syneron Bio reported nearly $100 million raised across its Series A and A+ rounds, with participation from AstraZeneca and multiple strategic and venture investors. Proceeds support its Synova high-throughput macrocyclic peptide discovery platform and advancement of pipeline programs toward clinical development. The combined financing amount is not a single round, and candidate-level oral clinical data were not disclosed.
Circle Pharma nominated CID-165, an orally available macrocyclic cyclin D1 RxL inhibitor, as the development candidate for its second oncology program. Preclinical studies supported disruption of the cyclin D1–Rb interaction and activity alone or with other therapies. Candidate nomination is a discovery-to-development milestone, not IND authorization or evidence that human dosing has begun.
PeptiDream described an orally administered macrocyclic peptide inhibiting IL-17A/A, A/F, and F/F. Preclinical challenge studies showed CXCL1 suppression and skin distribution. The company is progressing toward IND-enabling work and exploring partnerships. Entry into its development portfolio does not mean human dosing has begun, and claimed biologic-like activity remains preclinical.
MicroED identified two polymorphic structures of oxyacanthine dihydrochloride monohydrate in samples mislabeled as berbamine dihydrochloride. The forms differed principally in the conformation of a tetrahydroisoquinoline ring. Structural, energetic, and packing analyses suggested a thermodynamic preference between them. The study demonstrates how crystallographic analysis can expose both identity problems and polymorphism in complex natural-product samples.
3D ED/MicroED determined casopitant mesylate Forms 1 and 3 from one batch of fine powder containing an inseparable polymorphic mixture. Their structures differed through a small packing shift, explaining their very similar powder X-ray diffraction patterns. The work demonstrates how selecting individual microcrystals can resolve structurally similar phases that remain difficult to separate or distinguish in bulk measurements.
Biogen and Dayra announced a research collaboration to discover and optimize oral macrocyclic peptides for immunological targets. Dayra receives $50 million upfront and may receive candidate-acquisition payments and development milestones per program. Biogen would lead subsequent development, manufacturing, and potential commercialization. The agreement concerns early discovery rather than established clinical efficacy.
Sungening reported that its preclinical SG6001 oral cyclic peptide program for hyperlipidemia was included in Shenzhen’s strategic emerging industries support initiative for innovative drug technology. The announcement did not disclose an award amount or human results. Program support advances research resources rather than establishing clinical authorization, product approval, or completed commercial manufacturing.
Merck presented Phase 3 CORALreef HeFH results in adults with heterozygous familial hypercholesterolemia receiving background lipid-lowering therapy. Enlicitide reduced LDL-C by 59.4% versus placebo at week 24 and 61.5% at week 52. The overall safety profile was comparable with placebo. The study evaluated lipid changes rather than cardiovascular-event outcomes.
Merck reported Phase 3 CORALreef Lipids results showing a 55.8% placebo-adjusted LDL-C reduction at week 24 in the primary analysis. A post hoc reanalysis addressing biologically implausible baseline values estimated 59.7%. LDL-C reductions persisted through week 52. These lipid findings should not be equated with demonstrated reductions in cardiovascular events.
HitGen researchers describe a method for synthesizing DNA-encoded bicyclic peptides using cysteine-promoted cyclization and amide condensation under mild conditions. The abstract reports compatibility with varied sequences and ring sizes. This is discovery-platform chemistry, not evidence that the resulting peptides have oral exposure, clinical efficacy, or validated manufacturing-scale performance.
FDA approved oral linaclotide for irritable bowel syndrome with constipation in children ages 7 and older. Evidence included extrapolation from adult studies and a 12-week randomized pediatric trial. This gut-acting, disulfide-constrained peptide is not an example of high systemic oral absorption. Diarrhea remains an important adverse reaction, and use in children younger than 2 is contraindicated.
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