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Pharmacokinetics of a New Anti-HIV Agent VP-0510 and Development of its Amino Acid Prodrug for Improving Oral Bioavailability
2006
Cho, H.J. (Konkuk University, Seoul, Republic of Korea) | Choi, K.A. (Konkuk University, Seoul, Republic of Korea) | Sung, J.M. (Konkuk University, Seoul, Republic of Korea) | Jeong, S.M. (Konkuk University, Seoul, Republic of Korea) | Han, J.S. (Konkuk University, Seoul, Republic of Korea) | Kim, J.S. (Konkuk University, Seoul, Republic of Korea) | Shin, H.C. (Konkuk University, Seoul, Republic of Korea), E-mail: hshin@konkuk.ac.kr
We have studied pharmacokinetics of a new anti-human immunodeficiency virus (HIV) agent VP-0501 and its amino acid prodrug VP-0501AL which is designed to improve oral bioavailability. After oral administration at 100 mg/kg dose in rats (n=4), VP-0501 was not detectable in plasma (less than 50 ng/ml), while after the administration of VP-0501AL, VP-0501 was quantitatively detected, at least for 8 hrs, with Cmax of ca. 2.5 μg/ml and AUC of 8 hr*μg/ml.
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