Drug intelligence / Profile preview

prexasertib

Development stage
Phase 2
Lead developer
Acrivon Therapeutics
Modality
Small Molecules
01

Overview

Prexasertib is a small molecule inhibitor of checkpoint kinase 1 (CHK1) and, to a lesser extent, checkpoint kinase 2 (CHK2). By inhibiting these kinases, prexasertib disrupts DNA replication and repair processes in tumor cells, leading to accumulation of DNA damage, replication/mitotic catastrophe, and ultimately cell death. It has demonstrated antitumor activity as both monotherapy and in combination with chemotherapy or targeted agents. Prexasertib was originally developed by Array BioPharma and further developed by Eli Lilly; more recently it has been advanced by Acrivon Therapeutics for clinical development. The drug is being investigated primarily for the treatment of various cancers including platinum-resistant ovarian cancer, endometrial cancer, head and neck squamous cell carcinoma (HNSCC), anal cancer, neuroblastoma, rhabdomyosarcoma, acute myeloid leukemia (AML), myelodysplastic syndrome (MDS), medulloblastoma, breast cancer, prostate cancer (mCRPC), leukemia broadly defined as well as other solid tumors[1][3][4][5][6].

Other names
prexasertibLY2606368LY-2606368LY 2606368ACR368ACR-368ACR 368
02

Targets

CHEK1 (Checkpoint kinase 1)CHEK2 (Checkpoint kinase 2)RSK (RSK family)

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