Gilead Sciences, Inc.

Bristol-myers Squibb & Gilead Sciences, Inc.

Eidos Therapeutics, Inc.

Janssen Sciences Ireland Uc

Tobira Therapeutics, Inc.

Janssen R&d Ireland

Mark Michael Menning

Reza Oliyai

Terrence C Dahl

Taiyin Yang

Robert L Jerzewski

Munir A Hussain

Robert A Lipper

Jesper Alexis Jernelius

Sean Dalziel

Robert G Strickley

Richard Yu

Lauren Wiser

Joanna M Koziara

Brian P Kearney

Anita A Mathias

The present disclosure provides high-load tablet formulations of AG10 or a pharmaceutically acceptable salt thereof. In some aspects, provided herein are table formulations of AG10 or a pharmaceutically acceptable salt thereof that include at least 40% or more AG10 by weight and at least one pharmaceutical excipient selected from one or more fillers, one or more binders, one or more disintegrants, and one or more lubricants.

Formulations of AG10

The invention provides multilayer tablets that contain rilpivirine hydrochloride, emtricitabine, and tenofivir disoproxil fumarate. The tablets are useful for the treatment of HIV.

Therapeutic compositions comprising rilpivirine HCL and tenofovir disoproxil fumarate

The invention provides a composition comprising, a compound of formula (I): or a pharmaceutically acceptable salt thereof and a plurality of solid carrier particles, as well as methods for using the composition to inhibit the activity of cytochrome P-450.

Use of solid carrier particles to improve the processability of a pharmaceutical agent

The present invention relates to therapeutic combinations of [2-(6-amino-purin-9 yl)-1-methyl-ethoxymethyl]-phosphonic acid diisopropoxycarbonyloxymethyl ester (tenofovir disoproxil fumarate, Viread&#xae;) and (2R,5S,cis)-4-amino-5-fluoro-1-(2 hydroxymethyl-1,3-oxathiolan-5-yl)-(1H)-pyrimidin-2-one (emtricitabine, Emtriva&#x2122;, (&#x2212;)-cis FTC) and their physiologically functional derivatives. The combinations may be useful in the treatment of HIV infections, including infections with HIV mutants bearing resistance to nucleoside and/or non-nucleoside inhibitors. The present invention is also concerned with pharmaceutical compositions and formulations of said combinations of tenofovir disoproxil fumarate and emtricitabine, and their physiologically functional derivatives, as well as therapeutic methods of use of those compositions and formulations.

Compositions and methods for combination antiviral therapy

The present disclosure relates to novel crystalline salt forms of lamivudine, methods for the preparation thereof, pharmaceutical compositions thereof, and their use in the treatment of viruses such as Human Immunodeficiency Virus (HIV) infection.

Lamivudine salts

In accordance with this invention a novel pharmaceutical product containing efavirenz, emtricitabine and tenofovir DF are provided as a multicomponent unitary oral dosage form, component 1 comprising tenofovir DF (and, optionally, emtricitabine) and component 2 comprising efavirenz, wherein components 1 and 2 are in a stabilizing configuration. In preferred embodiments component 1 is made by dry granulation.

Unitary pharmaceutical dosage form

The present invention relates to therapeutic combinations of [2-(6-amino-purin-9-yl)-1-methyl-ethoxymethyl]-phosphonic acid diisopropoxycarbonyloxymethyl ester (tenofovir disoproxil fumarate, Viread&#xae;) and (2R,5S,cis)-4-amino-5-fluoro-1-(2-hydroxymethyl-1,3-oxathiolan-5-yl)-(1H)-pyrimidin-2-one (emtricitabine, Emtriva&#x2122;, (&#x2212;)-cis FTC) and their physiologically functional derivatives. The combinations may be useful in the treatment of HIV infections, including infections with HIV mutants bearing resistance to nucleoside and/or non-nucleoside inhibitors. The present invention is also concerned with pharmaceutical compositions and formulations of said combinations of tenofovir disoproxil fumarate and emtricitabine, and their physiologically functional derivatives, as well as therapeutic methods of use of those compositions and formulations.

In accordance with this invention a novel pharmaceutical product containing efavirenz, emtricitabine and tenofovir DF are provided as a multicomponent unitary oral dosage form, componentcomprising tenofovir DF (and, optionally, emtricitabine) and componentcomprising efavirenz, wherein componentsandare in a stabilizing configuration. In preferred embodiments componentis made by dry granulation.

This invention is directed to a composition comprising dry granulated tenofovir DF and emtricitabine, and a method for making same. Dry granulation was unexpectedly found to be important in preparing a tenofovir DF containing composition suitable for inclusion in a combination dosage form containing emtricitabine, efavirenz and tenofovir DF.

Method and composition for pharmaceutical product

The present invention relates to therapeutic combinations of [2-(6-amino-purin-9-yl)-1-methyl-ethoxymethyl]-phosphonic acid diisopropoxycarbonyloxymethyl ester (tenofovir disoproxil fumarate, Viread&#xae;) and (2R, 5S, cis)-4-amino-5-fluoro-1-(2-hydroxymethyl-1,3-oxathiolan-5-yl)-(1H)-pyrimidin-2-one(emtricitabine, Emtriva&#x2122;, (-)-cis FTC) and their physiologically functional derivatives. The combinations may be useful in the treatment of HIV infections, including infections with HIV mutants bearing resistance to nucleoside and/or non-nucleoside inhibitors. The present invention is also concerned with pharmaceutical compositions and formulations of said combinations of tenofovir disoproxil fumarate and emtricitabine, and their physiologically functional derivatives, as well as therapeutic methods of use of those compositions and formulations.

Growing community of inventors

San Francisco, CA, United States of America

Mark Michael Menning