Pharmaceutical Substances - Version 4.10
The version 4.10 of Pharmaceutical Substances was launched in April 2021.
Pharmaceutical Substances 4.10 contains 16 new APIs and a total of 45,248 structures, 12,834 reactions, and 2,779 active pharmaceutical ingredients.
Statement by the authors Prof. Axel Kleemann, Prof. Bernhard Kutscher and Dr. Dietmar Reichert
"This spring release describes 16 novel, innovative active pharmaceutical ingredients, some which have granted breakthrough therapy, fast track and orphan drug designation by the FDA.
The update covers two anti-COVID-19 agents. Colchicine is a tubulin polymerization inhibitor and was launched for the prevention of major inflammatory storm and reduction in risk of pulmonary complications due to severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) infection (COVID-19). Clofazimine was originally launched as antimycobacterial drug which has inhibitory SARS-CoV-2 activity by reducing viral load in the lung. It received orphan drug designation.
Promising new antitumor drugs were approved with Pralsetinib granted breakthrough therapy designation in the U.S. for the treatment of RET-mutation-positive MTC, Pexidartinib for treatment of adult patients with symptomatic tenosynovial giant cell tumor (TGCT), the marine cyclodepsipeptide Plitidepsin which has received orphan drug designation for the treatment of multiple myeloma and Lurbinectedin as an alkylating drug for treatment of metastatic small cell lung cancer (SCLC).
Breakthrough therapy designation also received five new drugs with the CFTR channel corrector Elexacaftor against cystic fibrosis, Eli Lilly´s oral 5-HT1F receptor agonist Lasmiditan as a first-in-class neurally acting anti-migraine agent and Fostemsavir for treatment HIV-1 infection in heavily treatment-experienced adults. The API has been granted fast track designation by the FDA. Eiger BioPharmaceuticals´oral prenylation inhibitor Lonafarnib was also granted breakthrough therapy designation for treatment of Hepatits D infections as well as La Jolla Pharmaceuticals´Artesunate for the treatment of severe malaria in adult and pediatric patients.
Furthermore the update contains the metalloproteinase inhibitor Abametapir for the topical treatment of head lice infestation, the beta3-adrenoreceptor agonist Vibegron for oral overactive bladder therapy and the Benzodiazepin Remimazolam as a GABA BZ site receptor agonist. Also described is Clascoterone as a 11-deoxycorticosterone-derived steroid ester for topical treatment for acne and the modified amino acid Acetylleucine for treatment of common inherited and acquired neurological diseases."
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- PDF Chemistry Catalog 2022 (PDF, 4 MB)