596365 Disclosed herein is a composition comprising pentamidine and oxaliplatin or irinotecan, and the use thereof in the treatment of a cancer, such as wherein the cancer is localized or metastatic pancreatic cancer, breast cancer, ovarian cancer, colon cancer, melanoma, leukemia, non-small cell lung cancer, CNS cancer, renal cancer or prostate cancer. Additionally disclosed is the use of pentamidine and leucovorin, oxaliplatin, and 5-fluorouracil, when the cancer patient has previously received a first-line chemotherapy comprising leucovorin, 5-fluorouracil and irinotocan or (b) leucovorin, 5-fluorouracil and irinotocan, when the cancer patient has previously received a first-line chemotherapy comprising leucovorin, oxaliplatin, and 5-fluorouracil, in the manufacture of a medicament for treating cancer in a cancer patient undergoing second-line chemotherapy.