Chemistry:Nemtabrutinib
From HandWiki
Short description: Chemical compound
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| Other names | MK-1026; ARQ 531 |
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| Formula | C25H23ClN4O4 |
| Molar mass | 478.93 g·mol−1 |
Nemtabrutinib (MK-1026, formerly ARQ 531) is a small molecule drug that works as a reversible Bruton's tyrosine kinase (BTK) inhibitor; unlike other BTK inhibitors it also works against some mutated forms of BTK.[1][2][3][4][5] Merck paid $2.7 billion to acquire the company ArQule and the drug, which is being investigated as a cancer treatment.[6]
References
- ↑ Sevindik, Ömür Gökmen; Chen, Chang; Yang, Jing; Farooqui, Mohammed Z.H.; Paszkiewicz-Kozik, Ewa (1 June 2023). "BELLWAVE-008: A phase 3 study of the efficacy and safety of nemtabrutinib in previously untreated patients (pts) with chronic lymphocytic leukemia (CLL)/small lymphocytic lymphoma (SLL) without TP53 aberrations.". Journal of Clinical Oncology 41 (16_suppl): TPS7594. doi:10.1200/JCO.2023.41.16_suppl.TPS7594.
- ↑ Woyach, J.; Flinn, I. W.; Awan, F. T.; Eradat, H.; Brander, D.; Tees, M.; Parikh, S. A.; Phillips, T. et al. (23 June 2022). "P682: Nemtabrutinib (Mk-1026), A Non-Covalent Inhibitor of Wild-Type and C481S Mutated Bruton Tyrosine Kinase for B-Cell Malignancies: Efficacy and Safety of the Phase 2 Dose-Expansion Bellwave-001 Study". HemaSphere 6: 578–579. doi:10.1097/01.HS9.0000845612.25766.0c.
- ↑ Reiff, Sean D.; Mantel, Rose; Smith, Lisa L.; Greene, J.T.; Muhowski, Elizabeth M.; Fabian, Catherine A.; Goettl, Virginia M.; Tran, Minh et al. (1 October 2018). "The BTK Inhibitor ARQ 531 Targets Ibrutinib-Resistant CLL and Richter Transformation". Cancer Discovery 8 (10): 1300–1315. doi:10.1158/2159-8290.CD-17-1409. PMID 30093506.
- ↑ Woyach, Jennifer A.; Flinn, Ian W.; Awan, Farrukh T.; Eradat, Herbert; Brander, Danielle; Tees, Michael; Parikh, Sameer A.; Phillips, Tycel J. et al. (15 November 2022). "Efficacy and Safety of Nemtabrutinib, a Wild-Type and C481S-Mutated Bruton Tyrosine Kinase Inhibitor for B-Cell Malignancies: Updated Analysis of the Open-Label Phase 1/2 Dose-Expansion Bellwave-001 Study". Blood 140 (Supplement 1): 7004–7006. doi:10.1182/blood-2022-163596.
- ↑ Woyach, Jennifer A.; Stephens, Deborah M.; Flinn, Ian W.; Bhat, Seema A.; Savage, Ronald E.; Chai, Feng; Eathiraj, Sudharshan; Reiff, Sean D. et al. (6 November 2023). "First in Human Study of the Reversible BTK Inhibitor Nemtabrutinib in Patients with Relapsed/Refractory Chronic Lymphocytic Leukemia and B-Cell Non-Hodgkin Lymphoma". Cancer Discovery. doi:10.1158/2159-8290.CD-23-0670. ISSN 2159-8290. PMID 37930156. https://pubmed.ncbi.nlm.nih.gov/37930156/.
- ↑ Lisa m. Jarvis (16 December 2019). "Merck will pay $2.7 billion for ArQule" (in en). C&EN Global Enterprise 97 (48): 13. doi:10.1021/cen-09748-buscon4. ISSN 2474-7408. https://pubs.acs.org/doi/10.1021/cen-09748-buscon4.
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