Drug intelligence / Profile preview

ormaplatin

Development stage
Unknown
Lead developer
National Cancer Institute
Modality
Small Molecules
Administration
Intravenous
01

Overview

**Ormaplatin** is a platinum (IV) analog antineoplastic agent developed for its altered toxicity profile and non-cross resistance to cisplatin in vitro and in vivo models[1][3][4][10]. It has demonstrated activity against cisplatin-resistant cell lines and undergoes conversion in extracellular environments to dichloro(D,L-trans)-1,2-diaminocyclohexaneplatinum(II) (PtCl2(trans-dach)), which is believed to be chiefly responsible for its cytotoxicity[4][10][7]. The drug was studied in phase I clinical trials for refractory solid tumors; its dose-limiting toxicities include peripheral sensory neuropathy and myelosuppression (primarily thrombocytopenia and granulocytopenia)[1][3]. It displayed high protein binding and linear pharmacokinetics, with moderate gastrointestinal toxicity (nausea, vomiting) and moderate myelosuppression[1][3]. Neurotoxicity is cumulative-dose dependent and may severely impact patient mobility at sufficient exposure[1]. Development was hampered due to neurotoxicity, and phase II dosing could not be pursued as a result[1][3]. No evidence found of regulatory approval or ongoing clinical development.

Brand names
tetraplatinormaplatin
Other names
tetraplatinNSC 363812NSC363812NSC-363812
02

Targets

DNA

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