Rocbrutinib

Rocbrutinib
Clinical data
Other names	HS-10561; LP-168; NWP-775
Legal status
Legal status	investigational;
Identifiers
	IUPAC name N-[5-[[6-[2-(4,4-dimethyl-9-oxo-1,10-diazatricyclo[6.4.0.02,6]dodeca-2(6),7-dien-10-yl)-3-(hydroxymethyl)-4-pyridinyl]-4-methyl-3-oxopyrazin-2-yl]amino]-2-[(2S)-2-methyl-4-(oxan-4-yl)piperazin-1-yl]phenyl]prop-2-enamide;
CAS Number	2485861-07-0;
PubChem CID	139416847;
IUPHAR/BPS	12875;
DrugBank	DB19445;
ChemSpider	129309149;
UNII	KD68L3GRW2;
ChEBI	CHEBI:759240;
ChEMBL	ChEMBL5314539;
Chemical and physical data
Formula	C42H51N9O5
Molar mass	761.928 g·mol−1
3D model (JSmol)	Interactive image;
	SMILES C[C@H]1CN(CCN1C2=C(C=C(C=C2)NC3=NC(=CN(C3=O)C)C4=C(C(=NC=C4)N5CCN6C7=C(CC(C7)(C)C)C=C6C5=O)CO)NC(=O)C=C)C8CCOCC8;
	InChI InChI=InChI=1S/C42H51N9O5/c1-6-37(53)45-32-20-28(7-8-34(32)49-14-13-48(23-26(49)2)29-10-17-56-18-11-29)44-38-41(55)47(5)24-33(46-38)30-9-12-43-39(31(30)25-52)51-16-15-50-35(40(51)54)19-27-21-42(3,4)22-36(27)50/h6-9,12,19-20,24,26,29,52H,1,10-11,13-18,21-23,25H2,2-5H3,(H,44,46)(H,45,53)/t26-/m0/s1; Key:OYJVFTNYBWVQHA-SANMLTNESA-N;

Rocbrutinib is an investigational new drug that is being evaluated by Newave Pharmaceuticals for the treatment of chronic lymphocytic leukaemia (CLL), diffuse large B cell lymphoma (DLBCL), and mantle cell lymphoma (MCL).^[1] It is a Bruton's tyrosine kinase (BTK) inhibitor.^[1]^[2]

Pharmacology

Rocbrutinib acts both as irreversible BTK inhibitor where its acrylamide reacts with cysteine 481 of BTK. It can also act as a reversible inhibitor of BTK that harbors the resistance C481S mutation.^[2]

Clinical trials

Rocbrutinib is currently in phase 3 clinical trials for mantle cell lymphoma.^[3]

References

1 2 "Rocbrutinib - Newave Pharmaceuticals". AdisInsight. Springer Nature Switzerland AG.
1 2 Benrashid S, Woyach JA (February 2026). "When Targeted Therapy Falls Short: Unraveling Resistance Mechanisms in Chronic Lymphocytic Leukemia". Current Hematologic Malignancy Reports. 21 (1) 6. doi:10.1007/s11899-026-00776-3. PMC 12935742. PMID 41741806.
↑ Clinical trial number NCT07377578 for "A Study of Rocbrutinib Versus Investigator's Choice of BTK Inhibitors in Patients With Relapsed or Refractory Mantle Cell Lymphoma" at ClinicalTrials.gov

[AdisInsight-1] 1 2 "Rocbrutinib - Newave Pharmaceuticals". AdisInsight. Springer Nature Switzerland AG.

[Benrashid_2026-2] 1 2 Benrashid S, Woyach JA (February 2026). "When Targeted Therapy Falls Short: Unraveling Resistance Mechanisms in Chronic Lymphocytic Leukemia". Current Hematologic Malignancy Reports. 21 (1) 6. doi:10.1007/s11899-026-00776-3. PMC 12935742. PMID 41741806.

[3] Clinical trial number NCT07377578 for "A Study of Rocbrutinib Versus Investigator's Choice of BTK Inhibitors in Patients With Relapsed or Refractory Mantle Cell Lymphoma" at ClinicalTrials.gov

[1]

[2]

[3]