Nemtabrutinib
Clinical data
Other namesMK-1026; ARQ 531
Legal status
Legal status
  • Investigational
Identifiers
CAS Number
PubChem CID
UNII
Chemical and physical data
FormulaC25H23ClN4O4
Molar mass478.93 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

  1. ↑ 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. S2CID 259080098.
  2. ↑ Woyach, J.; Flinn, I. W.; Awan, F. T.; Eradat, H.; Brander, D.; Tees, M.; Parikh, S. A.; Phillips, T.; Wang, W.; Reddy, N. M.; Farooqui, M. Z.; Byrd, J. C.; Stephens, D. M. (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. S2CID 250001988.
  3. ↑ Reiff, Sean D.; Mantel, Rose; Smith, Lisa L.; Greene, J.T.; Muhowski, Elizabeth M.; Fabian, Catherine A.; Goettl, Virginia M.; Tran, Minh; Harrington, Bonnie K.; Rogers, Kerry A.; Awan, Farrukh T.; Maddocks, Kami; Andritsos, Leslie; Lehman, Amy M.; Sampath, Deepa; Lapalombella, Rosa; Eathiraj, Sudharshan; Abbadessa, Giovanni; Schwartz, Brian; Johnson, Amy J.; Byrd, John C.; Woyach, Jennifer A. (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. PMC 6261467. PMID 30093506.
  4. ↑ Woyach, Jennifer A.; Flinn, Ian W.; Awan, Farrukh T.; Eradat, Herbert; Brander, Danielle; Tees, Michael; Parikh, Sameer A.; Phillips, Tycel J.; Ghori, Razi; Reddy, Nishitha M.; Farooqui, Mohammed Z.H.; Byrd, John C.; Stephens, Deborah M. (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. S2CID 256785160.
  5. ↑ Woyach, Jennifer A.; Stephens, Deborah M.; Flinn, Ian W.; Bhat, Seema A.; Savage, Ronald E.; Chai, Feng; Eathiraj, Sudharshan; Reiff, Sean D.; Muhowski, Elizabeth M.; Granlund, Lindsey; Szuszkiewicz, Lyndsey; Wang, Wayne; Schwartz, Brian; Ghori, Razi; Farooqui, Mohammed Z. H.; Byrd, John C. (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. S2CID 265032444.
  6. ↑ Lisa m. Jarvis (16 December 2019). "Merck will pay $2.7 billion for ArQule". C&EN Global Enterprise. 97 (48): 13. doi:10.1021/cen-09748-buscon4. ISSN 2474-7408. S2CID 212811804.
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