# US 12,594,244 B2 · Therapeutic compositions for treatment of human immunodeficiency virus

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- Number: US 12,594,244 B2
- Document ID: US12594244B2
- Status: Granted
- Kind: B2
- Application number: 19/343,371
- Filed: 2025-09-29
- Published: 2026-01-29
- Granted: 2026-04-07
- Earliest claimed: 2015-11-09
- Assignees: Gilead Sciences, Inc.
- Applicants: Gilead Sciences, Inc.
- Inventors: Benjamin Micah Collman; Lei Hong; Joanna M. Koziara
- Web page: https://patentgrep.com/patent/US12594244B2

## CPC

- A61K 9/209: {containing drug in at least two layers or in the core and in at least one outer layer}
- A61K 9/0053: {Mouth and digestive tract, i.e. intraoral and peroral administration}
- A61K 9/2013: {Organic compounds, e.g. phospholipids, fats}
- A61K 9/2027: {obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates}
- A61K 9/2054: {Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose}
- A61K 9/2086: {Layered tablets, e.g. bilayer tablets; Tablets of the type inert core-active coat (active cores with a complete drug-free outer coat A61K9/28)}
- A61K 9/2095: {Tabletting processes}
- A61K 9/28: Dragees; Coated pills or tablets {, e.g. with film or compression coating (A61K9/2072 takes precedence, e.g. partially coated tablets A61K9/2072, coated multilayer tablets A61K9/2086, tablets with drug-coated core A61K9/209)}
- A61K 9/2833: {Organic macromolecular compounds}
- A61K 31/513: having oxo groups directly attached to the heterocyclic ring, e.g. cytosine
- A61K 31/5365: ortho- or peri-condensed with heterocyclic ring systems
- A61K 31/537: spiro-condensed or forming part of bridged ring systems
- A61K 31/553: having at least one nitrogen and one oxygen as ring hetero atoms, e.g. loxapine, staurosporine
- A61K 31/675: having nitrogen as a ring hetero atom, e.g. pyridoxal phosphate
- A61P 31/18: for HIV
- A61K: PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES (devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms A61J3/00; chemical aspects of, or use of materials for deodorisation of air, for disinfection or sterilisation, or for bandages, dressings, absorbent pads or surgical articles A61L; soap compositions C11D)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS

## Abstract

A solid oral dosage form is provided, comprising a compound of Formula I or a pharmaceutically acceptable salt thereof, tenofovir alafenamide or a pharmaceutically acceptable salt thereof, and emtricitabine or a pharmaceutically acceptable salt thereof.

## Claims

### Claim 1

A tablet comprising from 6.5-11.0% w/w of a compound of Formula I:
or a pharmaceutically acceptable salt thereof, 3.0-4.5% w/w tenofovir alafenamide or a pharmaceutically acceptable salt thereof, and 25-30% w/w emtricitabine or a pharmaceutically acceptable salt thereof, where the weight percentages denote a proportion of the whole tablet.

### Claim 2

A tablet comprising from 7.0-11.0% w/w of a compound of Formula II:
3.5-4.1% w/w tenofovir alafenamide hemifumarate, and 25-30% w/w emtricitabine, where the weight percentages denote a proportion of the whole tablet.

### Claim 3 (depends on 1)

The tablet of claim 1, wherein the tablet does not contain lactose, crospovidone, or sodium stearyl fumarate.

### Claim 4 (depends on 1)

The tablet of claim 1, wherein the tablet further comprises croscarmellose sodium or magnesium stearate.

### Claim 5 (depends on 1)

The tablet of claim 1, wherein the tablet further comprises croscarmellose sodium, magnesium stearate, or microcrystalline cellulose.

### Claim 6 (depends on 1)

The tablet of claim 1, wherein the tablet releases at least about 50% of the compound of Formula I or the pharmaceutically acceptable salt thereof in about 20 minutes, measured using USP apparatus II, in 333 mL of fasted simulated intestinal fluid, pH 6.5, at 37° C. and paddle speed of 100 rpm.

### Claim 7 (depends on 6)

The tablet of claim 6, wherein the tablet releases at least about 60% of the compound of Formula I or the pharmaceutically acceptable salt thereof in about 20 minutes.

### Claim 8 (depends on 6)

The tablet of claim 6, wherein the tablet releases at least about 70% of the compound of Formula I or the pharmaceutically acceptable salt thereof in about 60 minutes.

### Claim 9

A tablet comprising:
(i) from about 6.4 w/w to about 8.5% w/w of a compound of Formula II
(ii) about 25% w/w to about 32% w/w emtricitabine,
(iii) about 3.5% w/w to about 4.5% w/w tenofovir alafenamide hemifumarate,
(iv) about 46% w/w to about 57% w/w microcrystalline cellulose,
(v) about 5.9% w/w to about 8.5% w/w croscarmellose sodium, and
(vi) about 1.0-2.0% w/w magnesium stearate.

### Claim 10 (depends on 9)

The tablet of claim 9, further comprising a film coating.

### Claim 11 (depends on 1)

The tablet of claim 1, wherein the tablet further comprises croscarmellose sodium and magnesium stearate.

### Claim 12 (depends on 1)

The tablet of claim 1, wherein the tablet further comprises croscarmellose sodium, magnesium stearate, and microcrystalline cellulose.

### Claim 13 (depends on 1)

The tablet of claim 1, wherein the tablet is a coated tablet.

### Claim 14 (depends on 1)

The tablet of claim 1, wherein the tablet has a total weight of between about 250 and about 750 mg.

### Claim 15 (depends on 2)

The tablet of claim 2, wherein the tablet does not contain lactose, crospovidone, or sodium stearyl fumarate.

### Claim 16 (depends on 2)

The tablet of claim 2, wherein the tablet further comprises croscarmellose sodium or magnesium stearate.

### Claim 17 (depends on 1)

The tablet of claim 1, wherein the tablet further comprises croscarmellose sodium and magnesium stearate.

### Claim 18 (depends on 2)

The tablet of claim 2, wherein the tablet further comprises croscarmellose sodium, magnesium stearate, or microcrystalline cellulose.

### Claim 19 (depends on 2)

The tablet of claim 2, wherein the tablet further comprises croscarmellose sodium, magnesium stearate, and microcrystalline cellulose.

### Claim 20 (depends on 2)

The tablet of claim 2, wherein the tablet is a coated tablet.

### Claim 21 (depends on 2)

The tablet of claim 2, wherein the tablet has a total weight of between about 250 and about 750 mg.

### Claim 22 (depends on 2)

The tablet of claim 2, wherein the tablet releases at least about 50% of the compound of Formula II in about 20 minutes, measured using USP apparatus II, in 333 mL of fasted simulated intestinal fluid, pH 6.5, at 37° C. and paddle speed of 100 rpm.

### Claim 23 (depends on 22)

The tablet of claim 22, wherein the tablet releases at least about 60% of the compound of Formula II in about 20 minutes.

### Claim 24 (depends on 22)

The tablet of claim 22, wherein the tablet releases at least about 70% of the compound of Formula II in about 60 minutes.

### Claim 25 (depends on 9)

The tablet of claim 9, wherein the tablet releases at least about 50% of the compound of Formula II in about 20 minutes, measured using USP apparatus II, in 333 mL of fasted simulated intestinal fluid, pH 6.5, at 37° C. and paddle speed of 100 rpm.

### Claim 26 (depends on 25)

The tablet of claim 25, wherein the tablet releases at least about 60% of the compound of Formula II in about 20 minutes.

### Claim 27 (depends on 25)

The tablet of claim 25, wherein the tablet releases at least about 70% of the compound of Formula II in about 60 minutes.

### Claim 28 (depends on 9)

The tablet of claim 9, wherein the tablet has a total weight of between about 250 and about 750 mg.

### Claim 29

A method of therapeutic treatment of an HIV infection comprising administering to a subject a tablet comprising:
(i) from about 6.4 w/w to about 8.5% w/w of the compound of Formula II
(ii) about 25% w/w to about 32% w/w emtricitabine,
(iii) about 3.5% w/w to about 4.5% w/w tenofovir alafenamide hemifumarate,
(iv) about 46% w/w to about 57% w/w microcrystalline cellulose,
(v) about 5.9% w/w to about 8.5% w/w croscarmellose sodium, and
(vi) about 1.0-2.0% w/w magnesium stearate.