setipiprant (ACT-129968) / J&J, AbbVie - LARVOL DELTA

Design, synthesis, and optimization of new indole acetic acid derivatives as potent and selective CRTH2 receptor antagonists: the discovery of ACT-774312. (PubMed, ChemMedChem) - "This compound which displayed a substantial improvement in potency in the presence of plasma versus setipiprant (ACT-129968) has exhibited an excellent overall pharmacokinetic profile. Further lead optimization to overcome a safety issue as observed in non-clinical studies with (S)-B-1 (ACT-453859), led to the discovery of the 4-azaindole derivative (S)-72 (ACT-774312) ((S)-2-(8-((5-chloropyrimidin-2-yl)(methyl)amino)-2-fluoro-6,7,8,9-tetrahydro-5H-pyrido[3,2-b]indol-5-yl)acetic acid) which was selected as a potential follow-up of setipiprant (ACT-129968)."

Journal • Allergy • Respiratory Diseases

Setipiprant for Androgenetic Alopecia in Males: Results from a Randomized, Double-Blind, Placebo-Controlled Phase 2a Trial. (PubMed, Clin Cosmet Investig Dermatol) - "No TESAEs were reported with setipiprant or finasteride. Setipiprant 1000 mg BID was safe and well tolerated but did not demonstrate efficacy versus placebo for scalp hair growth in men with AGA."

Clinical • P2a data • Alopecia • CNS Disorders • Dermatology • Multiple Sclerosis

J.P. Morgan Healthcare Conference (Actelion) - Setipiprant / Actelion; Anticipated P3 profiling study for allergic rhinitis in H1 2012

Anticipated P3 study

Phase 2A Study of Setipiprant Tablets in Androgenetic Alopecia in Males (clinicaltrials.gov) - P2a; N=169; Active, not recruiting; Sponsor: Allergan; Recruiting ➔ Active, not recruiting

Enrollment closed • Biosimilar

Efficacy, safety, and tolerability study of ACT-129968 in patients with seasonal allergic rhinitis (SAR) (clinicaltrials.gov) - P3, N=630; Not yet recruiting; New P3 trial

New trial • Asthma • Immunology

New drugs under investigation for the treatment of alopecias. (PubMed, Expert Opin Investig Drugs) - "In androgenetic alopecia, we are still looking for a topical treatment that is superior to topical minoxidil. However, stem-cell research is advancing and the goal to create new follicles or refresh dormant follicles may be realized in the near future."

Journal • Review