TABLE 1 | Camptothecin derivatives in clinical use

From the following article:

Topoisomerase I inhibitors: camptothecins and beyond

Yves Pommier

Nature Reviews Cancer 6, 789-802 (October 2006)


Camptothecin derivativeStatusRemarksIndications
Topotecan hydrochloride (Hycamtin)FDA approved (GlaxoSmithKline)Intravenous infusion (water-soluble)Metastatic ovarian cancer (second line); SCLC (second line)
Irinotecan hydrochloride (Camptosar)FDA approved (Pfizer*)Intravenous infusion (water-soluble)Metastatic colorectal cancer (first line with 5FU/leucovorin)
9-NC; Rubitecan (Orathecin)Phase II/III (SuperGen)Oral administration; converted to 9-ACPancreatic cancer
9-AC; IDEC-132Phase IIIntravenous infusion; oral; intraparenteralOvarian cancer (intraparenteral)
Exatecan mesylate (DX-8591f); DE-310Phase II/III (Daiichi)Intravenous infusionVarious carcinomas (sarcomas?)
Lurtotecan GI-147211 NX 211Phase II (Gilead)Intravenous infusion; liposomal (NX 211)Ovarian and other carcinomas
Gimatecan (ST-1481)Phase I/II (Novartis§)Oral administration; lipophilicGlioblastoma, SCLC and solid tumours
PEG–camptothecin; ProthecanPhase II (Enzon Inc.)PEGylated derivative; intravenous infusion (water-soluble)NSCLC and other solid tumours
Karenitecin; BNP-1350Phase II (Bionumerik Pharmaceuticals)Oral administration; lipophilicGlioblastomas, melanomas and NSCLC
Silatecan; DB-67PreclinicalLipophilicGlioblastomas
Diflomotecan; BN 80915Phase II (Ipsen)Intravenous infusionAdvanced metastatic cancers: colon, breast and prostate
*Licensed from Yakult Honsha Co. Ltd, Japan, and Daiichi Pharmaceutical Co. Ltd, Japan.
Licensed from Glaxo Wellcome.
§Licensed from Sigma-Tau.
Carboxymethyldextran polyalcohol carrier covalently linked through a peptidyl spacer. 5FU, 5-fluorouracil; FDA, US Food and Drugs Administration; NSCLC, non-small-cell lung cancer; PEG, poly(ethyleneglycol); SCLC, small-cell lung cancer.

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