mocetinostat
Overview
Mocetinostat (MGCD0103) is an orally available selective class I/IV histone deacetylase (HDAC) inhibitor targeting HDAC1, HDAC2, HDAC3, and HDAC11. It has been evaluated in hematologic malignancies and solid tumors including sarcomas, where HDAC inhibition is hypothesized to restore expression of silenced tumor suppressor genes and sensitize cells to cytotoxic agents.
Evidence in the corpus
- In a PDTO functional screen of 92 sarcoma specimens, mocetinostat + vinorelbine was one of five PDTO-matched treatment regimens applied in sarcoma patients; normalized organoid viability for this combination correlated with time-to-next-treatment across the n=5 matched-treatment cohort (R²=0.921, p=0.009) PMID:39305899.
- Mocetinostat is listed among the compounds tested across the sarcoma PDTO drug library, appearing as a component of combination regimens with clinical follow-up PMID:39305899.
- HDAC inhibitor mocetinostat completed Phase 2 accrual in metastatic urothelial carcinoma (NCT02236195); the TCGA MIBC analysis found chromatin-modifier mutations pervasive (10 of 39 SMGs) — predominantly inactivating — motivating this class of therapy PMID:28988769
Resistance mechanisms
- Not directly characterized in the corpus.
Cancer types (linked)
- Sarcoma (various histologies — mocetinostat + vinorelbine PDTO-matched treatment with clinical correlation)
Sources
- PMID:39305899 — Al Shihabi et al. 2024, Cell Stem Cell. Sarcoma PDTO functional precision-medicine screen; mocetinostat + vinorelbine as PDTO-matched treatment with R²=0.921 correlation with time-to-next-treatment.
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