Drug Class Detail

Drug Class BTK inhibitor

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Drug Name Trade Name Synonyms Drug Classes Drug Description
Ibrutinib Imbruvica PCI-32765 BTK inhibitor 20 EGFR Inhibitor (Pan) 38 HER2 Inhibitor 20 Imbruvica (ibrutinib) is a selective, irreversible inhibitor of Bruton's tyrosine kinase (BTK), which promotes apoptosis and inhibits B-cell mediated signaling pathways, and has additional activity against ERBB2 (HER2) and EGFR (PMID: 20615965, PMID: 21422473, PMID: 27678331). Imbruvica (Ibrutinib) is approved for mantle cell lymphoma and first line treatment of chronic lymphocytic leukemia (FDA.gov).
CNX-774 BTK inhibitor 20 CNX-774 is a small molecule that binds BTK and prevents its kinase activity (PMID: 24658273).
DTRMWXHS-12 DTRM-12 BTK inhibitor 20 DTRMWXHS-12 inhibits BTK, resulting in decreased B-cell receptor (BCR) signaling and potentially leading to reduced tumor cell growth (NCI Drug Dictionary).
RXC005 REDX08608 BTK inhibitor 20 REDX08608 is an inhibitor of BTK, which targets both wild-type and C481, thereby potentially resulting in inhibition of cell growth (Blood 2016 128:4399).
M7583 BTK inhibitor 20 M7583 inhibits BTK, which may result in decreased tumor growth (J Clin Oncol 35, 2017 (suppl; abstr e14101)).
RN486 BTK inhibitor 20 RN486 is a selective BTK inhibitor that inhibits proliferation of B-cells (PMID: 22228807).
GDC-0834 BTK inhibitor 20 GDC-0834 is a selective reversible inhibitor of BTK that inhibits B-cell proliferation and differentiation (PMID: 23958373, PMID: 25701252).
ONO-4059 ONO-GS-4059|ONO-WG-307 BTK inhibitor 20 ONO-4059 inhibits Bruton's Tyrosine Kinase (BTK), which leads to decreased B-cell proliferation and differentiation, and may have antitumor activity in B-cell malignancies (PMID: 23958373, PMID: 27776353).
CC-292 Spebrutinib AVL-292 BTK inhibitor 20 CC-292 (Spebrutinib) is a covalent inhibitor of Btk that decreases Btk kinase activity and activation of downstream signaling, resulting in reduced B-cell proliferation (PMID: 24518207).
Acalabrutinib Calquence ACP-196 BTK inhibitor 20 Calquence (acalabrutinib) selectively inhibits BTK, resulting in decreased B-cell receptor signaling, and potentially leading to decreased tumor cell proliferation (PMID: 27903679, PMID: 26957112). Calquence (acalabrutinib) is FDA approved for use in patients with mantle cell lymphoma (FDA.gov).
ARQ 531 BTK inhibitor 20 ARQ 531 is an ATP-competitive BTK inhibitor with activity against wild-type BTK and BTK C481S and has been demonstrated to inhibit migration and viability of chronic lymphocytic leukemia cells (ASH, Blood 2016 128:3232).
CG'806 BTK inhibitor 20 FLT3 Inhibitor 48 CG'806 is a small molecule multi-kinase inhibitor that inhibits both wild-type and mutant Flt3 and Btk, resulting in growth inhibition in tumor cells (Blood 2017 130:4629).
SNS-062 Vecabrutinib BTK inhibitor 20 Vecabrutinib (SNS-062) inhibits BTK, including BTK mutations associated with inhibitor resistance, which potentially results in decreased tumor growth (Mol Cancer Ther December 1 2015 (14) (12 Supplement 2) C186).
Dasatinib Sprycel BMS-354825 ABL Inhibitor (pan) 8 BCR-ABL Inhibitor 23 BTK inhibitor 20 CSF1R Inhibitor 22 DDR1 Inhibitor 8 DDR2 inhibitor 7 KIT Inhibitor 48 PDGFR Inhibitor (Pan) 27 SRC Inhibitor 26 TNK2 Inhibitor 6 Sprycel (dasatinib) is an inhibitor of the SRC-family of protein kinases, BCR-ABL, and ABL, and has additional activity against other kinases including KIT, DDR1/2, PDGFRA/B, and EPHA2, which prevents cell growth (PMID: 25709401, PMID: 25284748, PMID: 18797457). Sprycel (dasatinib) is FDA approved for both Philadelphia chromosome positive adult and pediatric chronic myelogenous leukemia and adult acute lymphoblastic leukemia (FDA.gov).
BGB-3111 Zanubrutinib BTK inhibitor 20 Zanubrutinib (BGB-3111) inhibits Bruton Tyrosine Kinase (BTK), leading to decreased B-cell activation and reduced growth of BTK over-expressing B-cells (NCI Drug Dictionary).
Bosutinib Bosulif SKI-606 ABL Inhibitor (pan) 8 AXL Inhibitor 24 BTK inhibitor 20 SRC Inhibitor 26 TNK2 Inhibitor 6 Bosulif (bosutinib) inhibits SRC and ABL kinases, and has additional activity against other kinases including AXL, TNK2, BTK, resulting in decreased pathway activation and inhibition of tumor cell proliferation (PMID: 12543790, PMID: 19039322, PMID: 26555154). Bosulif (bosutinib) is FDA approved for use in patients with Ph+ (BCR-ABL) chronic myelogenous leukemia (FDA.gov).
HM-71224 BTK inhibitor 20 HM-71224 is a small molecule inhibitor of BTK (PMID: 23958373).
LFM-A13 BTK inhibitor 20 JAK2 Inhibitor 17 LFM-A13 inhibits BTK, with additional activity against JAK2 and PLK, potentially resulting in increased tumor cell apoptosis (PMID: 17098432, PMID: 15196000, PMID: 10092645).
PLS-123 BTK inhibitor 20 PLS-123 is a selective irreversible inhibitor of BTK, which promotes apoptosis and inhibits proliferation of tumor cells (PMID: 25944695).
CGI1746 BTK inhibitor 20 CGI1746 binds to BTK and prevents its activation, resulting in decreased proliferation of B-cells (PMID: 21113169).
Molecular Profile Protein Effect Treatment Approaches