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.
ESSA Pharma presents the updated phase 1 Masofaniten clinical data at the 2024 ASCO Genitourinary Cancers Symposium. Masofaniten (EPI-7386) is a first-in-class investigational, N-terminal domain (NTD) androgen receptor (AR) inhibitor under development for prostate cancer. The androgen receptor (AR) signaling pathway is responsible for growth and survival of most prostate cancers. Unlike present therapies by binding to the ligand-binding domain (LBD) of AR and inducing drug resistance, Masofaniten offers a unique mechanism that inhibits AR activity through targeting the N-terminal domain (NTD) of the AR and suppresses AR transcriptional activation.
Masofaniten is studied with Enzalutamide in the phase 1/2 clinical trial for metastatic castration-resistant prostate cancer (mCRPC) patients on androgen deprivation therapy and naïve to second-generation antiandrogens.
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