SKI-2053R was launched in Korea for the treatment of patients with
advanced gastric adenocarcinoma. It is a third generation platinum complex
alkylating agent with less nephrotoxicity than cisplatin. In in vitro experiments,
SKI-2053R was highly active against various cell lines including cisplatinresistant
tumor cell lines. In mice implanted with L1210 cells, SKI-2053R
showed activity comparable or superior to cisplatin or carboplatin. In mice
implanted s.c. with human tumor xenograft KATO III (stomach adenocarcinoma),
SKI-2053R achieved growth-inhibition rates comparable with those of cisplatin.
General pharmacological studies in animals did not display any severe adverse
effects on the different systems at antitumour doses. Pharmacokinetic studies
after a single iv administration in rats demonstrated that the compound was
extensively and rapidly distributed into all tissues except the CNS. In patients with unresectable or metastatic gastric adenocarcinoma, SKI-2053R was active without significant hematological toxicity. Phase III trials with SKI-2053R are
currently ongoing for the treatment of various other cancers including lung, head
and neck.
Pharmaceutical Applications
heptaplatin is further examples of platinum-based agents being used in China and South
Korea, respectively. Heptaplatin
is used in South Korea to treat gastric cancer. It show the typical side effects such as
myelosuppression and mild hepatotoxicity. its success is limited and has not led to approval in the EU
or by the FDA.
