Drug intelligence / Profile preview

plitidepsin + cytarabine

Development stage
Preclinical
Lead developer
PharmaMar
Modality
Peptide-Drug Conjugates → Peptide Conjugates → Peptides, Small Molecules
Administration
Intravenous, Subcutaneous, Intrathecal
01

Overview

Plitidepsin + cytarabine is a combination of two antineoplastic agents used in oncology research and treatment. Plitidepsin is a cyclic depsipeptide originally isolated from the Mediterranean tunicate Aplidium albicans and developed by PharmaMar. It exerts its anticancer effects primarily by targeting eukaryotic elongation factor 1A2 (eEF1A2), leading to inhibition of cell growth and induction of apoptosis through mechanisms involving oxidative stress, activation of Rac1 GTPase, sustained activation of JNK and p38 MAPK pathways, and caspase-dependent apoptosis[2][6][8]. Plitidepsin also modulates the tumor microenvironment by affecting monocytes and nurse-like cells that support leukemic progression[2]. Cytarabine is a pyrimidine nucleoside analog classified as an antimetabolite. It inhibits DNA synthesis during the S phase of the cell cycle by being incorporated into DNA as its active triphosphate form (cytosine arabinoside triphosphate), thereby blocking DNA polymerase function and repair mechanisms[1][3][4]. This combination may be explored for synergistic effects in hematological malignancies such as leukemia.

Other names
Ara-CCytosar-U
02

Targets

POLA1 (DNA polymerase alpha)POLB (DNA polymerase beta)EEF1A2 (Eukaryotic elongation factor 1 alpha 2)RAC1 (Rac family small GTPase 1)JNK (Mitogen-activated protein kinase kinase kinase family)MAPK14 (p38 mitogen-activated protein kinase alpha)

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