title: Discovery of ursolic acid prodrug (NX-201): Pharmacokinetics and in vivo antitumor effects in PANC-1 pancreatic cancer.
abstract: The aim of our study was to develop ursolic acid (UA) prodrugs in order to overcome UA's weakness, which has an extremely low bioavailability. UA-medoxomil (NX-201), one of our UA prodrugs, showed an improved bioavailability about 200times better than UA in rodent model. According to in vivo test performed with PANC-1 xenograft SCID mouse model, tumor growth rate decreased dose-dependently and 100mg/kg dose of NX-201 had an anticancer effect comparable to gemcitabine. Most of all the combination of NX-201 (50mg/kg, po, daily) and gemcitabine (40mg/kg, iv, 2timesperweek) even reduced tumor size after three weeks.
authors: Nexoligo Co., Ltd., 40 4F 3408, Simin-daero 365 beongil, Dongan-gu, Anyang-si, Gyeonggi-do 14057, Republic of Korea; Department of Chemistry, Soongsil University, 369, Sangdo-ro, Dongjak-gu, Seoul 06978, Republic of Korea.
authors: Yeohong
authors: Y
authors: Yoon
authors: Nexoligo Co., Ltd., 40 4F 3408, Simin-daero 365 beongil, Dongan-gu, Anyang-si, Gyeonggi-do 14057, Republic of Korea.
authors: Jee Woong
authors: JW
authors: Lim
authors: Nexoligo Co., Ltd., 40 4F 3408, Simin-daero 365 beongil, Dongan-gu, Anyang-si, Gyeonggi-do 14057, Republic of Korea.
authors: Jiyoung
authors: J
authors: Kim
authors: KNOTUS Co., Ltd., 189, Dongureung-ro, Guri-si, Gyeonggi-do 02117, Republic of Korea.
authors: Younggi
authors: Y
authors: Kim
authors: Department of Chemistry, Soongsil University, 369, Sangdo-ro, Dongjak-gu, Seoul 06978, Republic of Korea.
authors: Keun Ho
authors: KH
authors: Chun
mesh_terms: D000818:Animals; D045744:Cell Line, Tumor; D006801:Humans; D016513:Mice, SCID; D010179:Pancreas / Q000187:drug effects* / Q000473:pathology; D010190:Pancreatic Neoplasms / Q000188:drug therapy* / Q000473:pathology; D011355:Prodrugs / Q000737:chemistry / Q000493:pharmacokinetics / Q000627:therapeutic use*; D014315:Triterpenes / Q000737:chemistry / Q000493:pharmacokinetics / Q000627:therapeutic use*; D023041:Xenograft Model Antitumor Assays; D000097245:Ursolic Acid
chemical_list: D011355:Prodrugs; D014315:Triterpenes; D000097245:Ursolic Acid
keywords: Anticancer; Bioavailability; Pancreatic cancer; Prodrug; Ursolic acid