Oral Irinotecan Hydrochloride Formulation VAL-413

**Semantic type:** Organic Chemical|Pharmacologic Substance

**Definition:** An orally bioavailable flavored formulation composed of the hydrochloride salt form of irinotecan, a semisynthetic derivative of camptothecin, with potential antineoplastic activity. Upon oral administration of oral irinotecan HCl formulation VAL-413, irinotecan is converted to the biologically active metabolite 7-ethyl-10-hydroxy-camptothecin (SN-38) by a carboxylesterase-converting enzyme. In turn, SN-38 inhibits topoisomerase I activity by stabilizing the cleavable complex of topoisomerase I and DNA, resulting in DNA breaks. This results in an inhibition of DNA replication and an induction of apoptosis in cancer cells. VAL-413 may improve tolerability of oral irinotecan and improve compliance.

**Synonyms:** - Oral Irinotecan HCl Formulation VAL-413 - Oral Irinotecan VAL-413 - Orotecan - VAL 413 - VAL-413 - VAL413