Use of a Sulfonamide Compound For Improving the Pharmacokinetics of a Drug
AssigneeTibotec Pharmaceuticals Ltd.
InventorsGerben Albert Eleutherius Van 'T Klooster, Piet Tom Bert Paul Wigerinck, Sandra De Meyer, Lieven Elvire Colette Baert, Herman Augustinus De Kock
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Abstract
A method for improving the pharmacokinetics of drugs, which are metabolized by cytochrome P450 monooxygenase is disclosed. More specifically it relates to a method for improving the pharmacokinetics of retroviral protease inhibitors and in particular for improving the pharmacokinetics of human immunodeficiency virus (HIV) protease inhibitors. A pharmaceutical composition and its use in the manufacture of a medicament for the inhibition or treatment of an HIV infection or AIDS in a human being are also part of the invention.
Claims19
A method of improving the pharmacokinetic properties of a drug, said method comprising the administration of a compound having the formula
- an N-oxide, salt, stereo-isomeric form or prodrug thereof wherein X represents S;
- Y represents OH;
- R1 represents hydrogen;
- R2 is phenyl;
- R3 is iso-butyl;
- R4 is hydrogen and R5 is hydrogen.
A pharmaceutical composition comprising a compound having the chemical name 5-thiazolylmethyl[(1S,2R)-3[[(2-amino-6-benzoxazolyl)sulfonyl](2-methylpropyl)amino]-2-hydroxy-1-(phenylmethyl)propyl]carbamate, a pharmaceutically acceptable carrier and a drug which is metabolized by cytochrome P450 and wherein said drug is a HIV protease inhibitor selected from the group consisting of darunavir, amprenavir, fosamprenavir, ritonavir, nelfinavir, saquinavir, indinavir, lopinavir, lasinavir, atazanavir, BMS 186318, DPC 681, DPC 684, tipranavir, AG1776, DMP 450, L 756425, PD178390, PNU 140135 or glycosylation inhibitors such as castanospermine, deoxynojirimycine.
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A method for improving the pharmacokinetics of a drug which is metabolized by cytochrome P450 comprising administering to a human host in need of such treatment a therapeutically effective amount of a combination of said drug or a pharmaceutically acceptable salt thereof and a compound compound having the formula
- an N-oxide, salt, stereo-isomeric form or prodrug thereof wherein X represents S;
- Y represents OH;
- R1 represents hydrogen;
- R2 is phenyl;
- R3 is iso-butyl;
- R4 is hydrogen and R5 is hydrogen.
Dependencies are inferred from the claim text.