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Bioorg Med Chem Lett. 2016 Nov 15;26(22):5524-5527. doi: 10.1016/j.bmcl.2016.10.008. Epub 2016 Oct 6.

Discovery of ursolic acid prodrug (NX-201): Pharmacokinetics and in vivo antitumor effects in PANC-1 pancreatic cancer.

Author information

1
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.
2
Nexoligo Co., Ltd., 40 4F 3408, Simin-daero 365 beongil, Dongan-gu, Anyang-si, Gyeonggi-do 14057, Republic of Korea.
3
KNOTUS Co., Ltd., 189, Dongureung-ro, Guri-si, Gyeonggi-do 02117, Republic of Korea.
4
Department of Chemistry, Soongsil University, 369, Sangdo-ro, Dongjak-gu, Seoul 06978, Republic of Korea.

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.

KEYWORDS:

Anticancer; Bioavailability; Pancreatic cancer; Prodrug; Ursolic acid

PMID:
27769622
DOI:
10.1016/j.bmcl.2016.10.008
[Indexed for MEDLINE]

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