Drug intelligence / Profile preview

leflunomide + mitoxantrone + prednisone

Development stage
Unknown
Lead developer
Pfizer
Modality
Small Molecules
Administration
Oral (leflunomide, Prednisone), Intravenous (mitoxantrone, Investigational Leflunomide)
01

Overview

This combination consists of three drugs: **leflunomide**, **mitoxantrone**, and **prednisone**. - **Leflunomide** is an isoxazole immunosuppressive drug that inhibits pyrimidine synthesis and suppresses the proliferation of T and B lymphocytes by inhibiting dihydroorotate dehydrogenase. It is primarily used as a disease-modifying therapy in autoimmune diseases and has reported efficacy in myasthenia gravis and primary membranous nephropathy[1][2][3]. - **Mitoxantrone** is an anthracenedione antineoplastic agent with immunosuppressive properties. It works mainly through DNA intercalation and inhibition of topoisomerase II, preventing DNA synthesis and cell division, often used in cancer and some autoimmune conditions[3]. - **Prednisone** is a synthetic corticosteroid prodrug (converted in vivo to prednisolone) that suppresses immune system activity and inflammation by glucocorticoid receptor activation, thereby modulating transcription of anti-inflammatory and immunosuppressive proteins[1][2][3]. As a combination, these agents have been studied experimentally, particularly in the context of cancer (notably hormone-refractory prostate cancer), myasthenia gravis, and immunologic kidney diseases, to enhance immunosuppression or antitumor efficacy while aiming to balance efficacy and toxicity[1][2][3]. No universally approved fixed-dose or co-formulated product comprising all three agents exists, but regimens combining them are present in some clinical trial protocols.

02

Targets

GR (Glucocorticoid receptor)DHODH (Dihydroorotate dehydrogenase (quinone), mitochondrial)TOP2A (DNA topoisomerase II)

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