Drug intelligence / Profile preview

transplatin

Development stage
Discontinued
Modality
Small Molecules
Administration
Intravenous
01

Overview

**Transplatin** is the trans isomer of dichlorodiammineplatinum(II), a coordination complex of platinum with two chloride and two ammonia ligands in a square planar geometry. It is a pale yellow solid with low water solubility and is distinct from its cis isomer, cisplatin, which is an important anticancer drug. Transplatin is clinically ineffective as an anticancer agent. Mechanistically, transplatin forms DNA adducts preferentially leading to interstrand crosslinks and monoadducts rather than the 1,2-intrastrand crosslinks characteristic for cisplatin[2][4][7]. These transplatin-induced DNA lesions are more readily repaired by cellular mechanisms, and transplatin is subject to inactivation by cellular nucleophiles (e.g., glutathione), contributing to its lack of anticancer efficacy[7]. Replacement of the ammonia ligands with other groups has led to transplatin-derived drugs with some promising antitumor activity, but native transplatin itself is clinically inactive[2][3][7].

Other names
transplatintrans-dichlorodiammineplatinum(II)trans-diamminedichloroplatinumtrans-PtCl2(NH3)2
02

Targets

DNA

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