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Tulmimetostat is an experimental tablet that blocks the gene-silencing enzymes EZH1 and EZH2. Novartis gained it by buying MorphoSys in 2024 and is testing it in prostate cancer, lymphomas and other solid tumours.
Tulmimetostat (CPI-0209, DZR123) is an oral dual inhibitor of EZH1 and EZH2 taken once a day, as described in its registry records. It came to Novartis with the acquisition of MorphoSys in 2024. Novartis's phase 1/2 trial (NCT04104776), running since 2019, enrols people with advanced solid tumours and lymphomas, including diffuse large B-cell lymphoma, T-cell lymphoma, mesothelioma, castration-resistant prostate cancer and endometrial cancer. In prostate cancer, TulmiSTAR-01 (NCT07206056) combines it with luxdegalutamide in metastatic castration-resistant disease and TulmiSTAR-02 (NCT07190300) with darolutamide or abiraterone in metastatic hormone-sensitive disease. Investigator-led trials test it with carboplatin in recurrent ovarian cancer (NCT05942300), alone in mycosis fungoides and Sézary syndrome (NCT05944562) and with pembrolizumab in non-small cell lung cancer (NCT05467748). No results are recorded here.
A tablet that blocks EZH2 and its close relative EZH1, enzymes that switch genes off by marking the proteins DNA is wound around. Blocking them can switch back on genes that hold cancer growth in check. Connects to EZH2.
1.Tulmimetostat slips into a pocket on EZH2.
Background: ADC sequencing, Antigen escape (antigen loss, lineage switch), BCG-unresponsive, Castration-resistant prostate cancer (CRPC), Circulating tumour DNA (ctDNA). Also on OnCo: Resistance: how tumours escape each drug class · Lines of therapy.
| Date | Deal | Type | Upfront | Total | Source |
|---|---|---|---|---|---|
| 2024-02-05 | MorphoSys (Novartis) to Novartis Pelabresib (BET inhibitor) and tulmimetostat | Acquisition | not disclosed | €2.7bn | source |
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Query for this drug: (TITLE:"Tulmimetostat" OR ABSTRACT:"Tulmimetostat" OR TITLE:"DZR123" OR ABSTRACT:"DZR123" OR TITLE:"CPI-0209" OR ABSTRACT:"CPI-0209") AND (cancer OR tumor OR tumour OR oncology OR carcinoma OR lymphoma OR leukemia OR leukaemia OR myeloma OR sarcoma OR melanoma OR glioma). Results are unfiltered search hits about Tulmimetostat, not a curated reading list.
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