Drug intelligence / Profile preview

levoleucovorin + pralatrexate

Development stage
Unknown
Lead developer
Assertio
Modality
Small Molecules
Administration
Intravenous, Oral
01

Overview

levoleucovorin + pralatrexate is a combination of two agents: **levoleucovorin**, the pharmacologically active (6S) diastereomer of folinic acid, and **pralatrexate**, a folate analog antimetabolite. Levoleucovorin is used as a rescue therapy to diminish toxic effects of folic acid antagonists by bypassing the inhibition of dihydrofolate reductase (DHFR) and supplying tetrahydrofolate directly for cellular processes. Pralatrexate is a chemotherapeutic agent that selectively inhibits DHFR, thereby blocking DNA and RNA synthesis and causing cancer cell death, especially in rapidly dividing cells. In some clinical studies and case reports, levoleucovorin (or leucovorin) is used adjunctively with pralatrexate to mitigate mucositis and other toxicities associated with pralatrexate therapy, especially in peripheral T-cell lymphoma and cutaneous T-cell lymphoma. While not a fixed-dose combination with a unique brand name, this combination reflects clinical practice of concomitant or prophylactic levoleucovorin use with pralatrexate for toxicity management in chemotherapy regimens[3][5][6].

02

Targets

DHFR (Dihydrofolate reductase)FPGS (Folylpolyglutamate synthase, mitochondrial)RFC1 (Reduced folate carrier type 1)

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