Drug intelligence / Profile preview

TLK286 + cisplatin

Development stage
Unknown
Lead developer
Telik
Modality
Peptide-Drug Conjugates → Peptide Conjugates → Peptides, Small Molecules
Administration
Intravenous
01

Overview

TLK286 (also known as TELCYTA) is a glutathione analog prodrug that is activated by the enzyme glutathione S-transferase P1-1 (GST P1-1), which is often overexpressed in certain cancers such as non-small cell lung cancer and ovarian carcinoma. Upon activation, TLK286 induces apoptosis in tumor cells. It has demonstrated activity as a single agent in chemotherapy-resistant ovarian cancer and platinum-resistant non-small cell lung cancer[2][6]. Cisplatin is a platinum-based chemotherapy drug classified as an alkylating agent. It works by cross-linking DNA strands to prevent replication and transcription, leading to apoptosis of rapidly dividing tumor cells[3][4]. The combination of TLK286 with cisplatin has been studied for synergistic effects in advanced cancers such as non-small cell lung cancer and ovarian carcinoma; the synergy may be mediated through modulation of glutathione/GST resistance pathways[6]. Both drugs are administered intravenously.

Brand names
Platinol-AQPlatinol
Other names
cis-diamminedichloroplatinum(II)TLK286TLK-286TLK 286
02

Targets

GSTP1 (Glutathione S-transferase P)DNA

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