Pharmaceutical Substances - Version 4.12

The version 4.12 of Pharmaceutical Substances was launched in April 2022.

This spring release covers 14 new APIs and presents quite a few first-in-class drug products with innovative mechanism of action as well as fast track or breakthrough designation.


Amongst them is  nirmatrelvir (Paxlovid™), an antiviral SARS-CoV-2 3CL protease inhibitor developed by Pfizer, consisting of co-packaged nirmatrelvir tablets with ritonavir tablets. The compound is co-administered with a low dose of ritonavir to slow its metabolism so that it remains active in the body for longer periods of time at higher concentrations.


Promising new kinase inhibitors were approved with asciminib against Philadelphia chromosome-positive chronic myeloid leukemia (Ph+ CML) and belumosudil for treatment of chronic graft-versus-host disease (cGVHD) acting as a rho kinase 2 (ROCK 2) inhibitor. In 2021, breakthrough therapy designation was granted in the U.S. for both these novel drugs.


Breakthrough designation was also received by the new drug bulevirtide against Hepatitis D as a viral entry-inhibiting peptide that inhibits the NTCP receptor.


New drugs against progressive familial intrahepatic cholestasis (PFIC) such as odevixabat and maralixibat were covered in this update as the first oral ileal bile acid transporter (IBAT) inhibitors.


Further progress was also achieved by plerixafor as a first generation drug to enhance mobilization of hematopoietic stem cells for transplantation in patients with multiple myeloma, by sapropterin for the treatment of atypical hyperphenylalaninemia (HPA)/phenylketonuria, and by lefamulin, a semi-synthetic pleuromutilin antibiotic.


Furthermore, the update contains osilodrostat for treatment of Cushing's disease and avacopan, an oral small-molecule C5aR antagonist for treatment of microscopic polyangiitis, as new drugs. Additionally, you will find new entries such as the female contraceptive estetrol as well as voclosporin for treatment of adult patients with active lupus nephritis, and floxuridine, an antimetabolite used against colorectal cancer, as well as an update to menthol in this latest release.


Prof. A. Kleemann     Prof. B. Kutscher     Dr. D. Reichert



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