Nemtabrutinib Explained

Drug Name:	Nemtabrutinib
Synonyms:	MK-1026; ARQ 531
Legal Status:	Investigational
Cas Number:	2095393-15-8
Unii:	JTZ51LIXN4
Pubchem:	129045720
C:	25
H:	23
Cl:	1
N:	4
O:	4

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]

Notes and References

1. Sevindik . Ömür Gökmen . Chen . Chang . Yang . Jing . Farooqui . Mohammed Z.H. . Paszkiewicz-Kozik . Ewa . 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 . 1 June 2023 . 41 . 16_suppl . TPS7594 . 10.1200/JCO.2023.41.16_suppl.TPS7594. 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. . 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 . 23 June 2022 . 6 . 578–579 . 10.1097/01.HS9.0000845612.25766.0c. 250001988 . free .
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. . The BTK Inhibitor ARQ 531 Targets Ibrutinib-Resistant CLL and Richter Transformation . Cancer Discovery . 1 October 2018 . 8 . 10 . 1300–1315 . 10.1158/2159-8290.CD-17-1409. 30093506 . 6261467 . free .
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. . 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 . 15 November 2022 . 140 . Supplement 1 . 7004–7006 . 10.1182/blood-2022-163596. 256785160 . free .
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. . 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 . 6 November 2023 . 10.1158/2159-8290.CD-23-0670 . 37930156 . 265032444 . 2159-8290.
6. Merck will pay $2.7 billion for ArQule . C&EN Global Enterprise . 16 December 2019 . 97 . 48 . 13 . 10.1021/cen-09748-buscon4 . en . 2474-7408 . Lisa m. Jarvis . 212811804 .