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VIP152 + bruton's tyrosine kinase inhibitor

Development stage
Unknown
Lead developer
Vincerx
Modality
Small Molecules
Administration
Oral (for Btk Inhibitors Such As Ibrutinib, Acalabrutinib, Zanubrutinib, Pirtobrutinib)[2][6], Intravenous (for VIP152)[1][3][5]
01

Overview

VIP152 + bruton's tyrosine kinase inhibitor is an experimental combination therapy consisting of VIP152, a highly selective and potent cyclin-dependent kinase 9 (CDK9) inhibitor, and a Bruton's tyrosine kinase (BTK) inhibitor (exact BTK inhibitor unspecified in the provided context). VIP152 is a small molecule that blocks CDK9 activity, resulting in the downregulation of oncogenic drivers such as MYC and MCL1, which play crucial roles in certain hematologic malignancies and solid tumors. Approved BTK inhibitors include ibrutinib, acalabrutinib, zanubrutinib, and pirtobrutinib, all of which inhibit the BTK pathway to disrupt B-cell receptor signaling critical for the proliferation and survival of malignant B cells. The rationale for their combination centers on complementary mechanisms of action aimed at overcoming resistance and improving outcomes in cancers such as chronic lymphocytic leukemia (CLL) and other B-cell malignancies[1][3][4][5][6].

Other names
BAY 1251152 + bruton's tyrosine kinase inhibitor
02

Targets

ERBB2 (Erb-b2 receptor tyrosine kinase 2)CDK7ABL1 (ABL proto-oncogene 1, non-receptor tyrosine kinase)IRAK1 (Interleukin-1 receptor-associated kinase 1)PIKFYVE (Phosphoinositide kinase, FYVE-type zinc finger containing enzyme)GSK3 (Glycogen synthase kinase 3 beta)CDK9 (Cyclin-dependent kinase 9)

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