Drug intelligence / Profile preview

dociparstat + cytarabine + idarubicin

Development stage
Unknown
Lead developer
Jazz Pharmaceuticals
Modality
Bivalent/Multivalent Binders → Multivalent & Scaffold-Based Small Molecules → Small Molecules
Administration
Intravenous
01

Overview

This is a combination regimen of **dociparstat**, **cytarabine**, and **idarubicin**. - **Dociparstat** (also known as DSTAT, previously known as CX-01) is a glycosaminoglycan derivative of heparin, modified to limit anticoagulant activity while preserving anti-inflammatory and anti-leukemia properties. Its primary mechanism is inhibition of high mobility group box 1 (HMGB1) and interactions with selectins; it also disrupts signaling involved in leukemic cell survival and migration. - **Cytarabine** is a pyrimidine analog antimetabolite that is phosphorylated intracellularly and incorporated into DNA, thereby inhibiting DNA synthesis and function. It is a mainstay of acute myeloid leukemia (AML) induction chemotherapy and is cytotoxic to rapidly dividing hematopoietic cells[3]. - **Idarubicin** is an anthracycline antibiotic that intercalates into DNA and inhibits topoisomerase II, leading to DNA strand breaks and impairment of DNA replication and transcription, with resultant apoptosis of rapidly dividing cells. It has major utility in AML induction[2][6][7][9]. This regimen is under investigation for the treatment of **acute myeloid leukemia (AML)**, particularly in attempts to improve induction outcomes through dociparstat’s additional anti-inflammatory and anti-leukemic properties. The use of dociparstat in this combination is not standard of care; the standard backbone for AML remains idarubicin + cytarabine[7][9]. Dociparstat-containing regimens are being evaluated in clinical trials for AML.

02

Targets

HMGB1 (High mobility group protein B1)DNA polymerase familyCXCL12 (C-X-C motif chemokine ligand 12)TOP2A (DNA topoisomerase II)DNASELP (P-selectin)

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