Combination therapy
The present invention relates to a combination therapy for treating an HIV infection or inhibiting integrase comprising (S)-6-(3-Chloro-2-fluorobenzyl)-1-(1-hydroxymethyl-2-methylpropyl)-7-methoxy-4-oxo-1,4-dihydroquinoline-3-carboxylic acid (“Compound A”) or a pharmaceutically acceptable solvate or salt thereof in combination with at least one other anti-HIV agent. In some embodiments of the present invention, the other anti-HIV agents are chosen from reverse transcriptase inhibitors and protease inhibitors. In certain embodiments of the present invention, the other anti-HIV agents are chosen from AZT, 3TC, PMPA, efavirenz, indinavir, nelfinavir, a combination of AZT/3TC, and a combination of PMPA/3TC. Since Compound A has a high inhibitory activity specific for integrases, when used in combinations with other anti-HIV agents it can provide a combination therapy with fewer side effects for humans.
1. A method for treating an HIV infectious disease in a human patient comprising administering to the patient a combination of:
(a) an effective amount of (S)-6-(3-Chloro-2-fluorobenzyl)-1-(1-hydroxymethyl-2-methylpropyl)-7-methoxy-4-oxo-1,4-dihydroquinoline-3-carboxylic acid or a pharmaceutically acceptable solvate or salt thereof,
(b) an effective amount of tenofovir disoproxil fumarate, and
(c) an effective amount of emtricitabine.
2. The method of claim 1 , wherein (a) and (b) and (c) are formulated together and administered as a single therapeutic composition.
3. A method for treating an HIV infectious disease in a human patient comprising administering to the patient a combination of:
(a) an effective amount of (S)-6-(3-Chloro-2-fluorobenzyl)-1-(1-hydroxymethyl-2-methylpropyl)-7-methoxy-4-oxo-1,4-dihydroquinoline-3-carboxylic acid or a pharmaceutically acceptable solvate or salt thereof,
(b) an effective amount of GS-7340, and
(c) an effective amount of emtricitabine.
4. The method of claim 3 , wherein (a) and (b) and (c) are formulated together and administered as a single therapeutic composition.
5. A composition for treating an HIV infectious disease in a human patient comprising:
(a) an effective amount of (S)-6-(3-Chloro-2-fluorobenzyl)-1-(1-hydroxymethyl-2-methylpropyl)-7-methoxy-4-oxo-1,4-dihydroquinoline-3-carboxylic acid or a pharmaceutically acceptable solvate or salt thereof,
(b) an effective amount of tenofovir disoproxil fumarate, and
(c) an effective amount of emtricitabine.
6. A composition for treating an HIV infectious disease in a human patient comprising:
(a) an effective amount of (S)-6-(3-Chloro-2-fluorobenzyl)-1-(1-hydroxymethyl-2-methylpropyl)-7-methoxy-4-oxo-1,4-dihydroquinoline-3-carboxylic acid or a pharmaceutically acceptable solvate or salt thereof,
(b) an effective amount of GS-7340, and
(c) an effective amount of emtricitabine.