Pyrimidine, also known as 1,3-diazobenzene, is a heterocyclic compound with the chemical formula C4H4N2. Pyrimidine is formed by substituting 2 nitrogen atoms for 2 carbons in the meta-position of benzene. It is a diazine and retains its aromaticity. Derivatives of pyrimidine widely exist in organic macromolecular nucleic acids, and many drugs also contain pyrimidine rings. In nucleic acids, three nucleobases are pyrimidine derivatives: cytosine, thymine and uracil. There are a variety of pyrimidine-containing drugs on the market, most of which are kinase inhibitors.
U.S. FDA approved Pfizer's BRAFTOVI® (Encorafenib) + MEKTOVI® (Binimetinib) for the treatment of adult patients with metastatic non-small cell lung cancer (NSCLC) with a BRAF V600E mutation. The FDA's approval is based on data from the ongoing Phase 2 PHAROS clinical trial. Encorafenib is an oral small molecule BRAF kinase inhibitor, and Binimetinib is an oral small molecule MEK inhibitor targeting key proteins in the MAPK signaling pathway (RAS-RAF-MEK-ERK). Chemenu has been working to develop more compounds for drug discovery. Here are the building blocks we can provide.
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