Drug intelligence / Profile preview

zalypsis

Development stage
Phase 2
Lead developer
PharmaMar
Modality
Metabolically Activated Prodrugs → Prodrugs/Conditional Activator Small Molecules → Small Molecules, Classical Binding Small Molecules → Small Molecules, Nucleic Acid-Directed Small Molecules → Small Molecules
Administration
Intravenous
01

Overview

Zalypsis is a semi-synthetic tetrahydroisoquinoline alkaloid structurally related to marine-derived compounds such as jorumycin and ecteinascidins. It acts as a DNA-binding agent that covalently binds to the minor groove of DNA, preferentially at guanine-rich sequences. This interaction leads to inhibition of transcription and cell cycle progression, induction of S-phase arrest, double-stranded DNA breaks (DSBs), and ultimately apoptosis in tumor cells[1][3][6]. Zalypsis has demonstrated potent antitumor activity in preclinical models across various solid tumors and hematological malignancies including multiple myeloma and acute myeloid leukemia[1][3][6][8]. The drug has been evaluated in phase I/II clinical trials for diseases such as lymphoma, solid tumors, Ewing's sarcoma, endometrial cancer, uterine cervical cancer, and multiple myeloma[2][7]. Its development status remains investigational.

Brand names
Zalypsis
Other names
synthetic alkaloid PM00104tetrahydroisoquinoline alkaloid PM00104
02

Targets

DNA

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