IP Library › Granted Patent US 12678408
Granted Patent B2
US 12678408 · App. 19/545,594 · Granted Jul 14, 2026

Pharmaceutical formulations comprising tenofovir alafenamide and emtricitabine

Inventors: Joanna M. Koziara (Foster City, CA); Scott McCallister (San Francisco, CA)
Assignee: Gilead Sciences, Inc.
A61K9/2054A61K9/0053A61K9/2013A61K9/209A61K9/284A61K9/2866A61K31/513A61K31/675
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Quick Facts
Patent No.
US 12678408
App. No.
19/545,594
Granted
Jul 14, 2026
Kind
B2
Abstract

The invention provides a solid oral dosage form comprising tenofovir alafenamide or a pharmaceutically acceptable salt thereof, and emtricitabine or a pharmaceutically acceptable salt thereof.

Claims (83)

1 . A tablet, consisting of:

(a) 25 mg tenofovir alafenamide, or a pharmaceutically acceptable salt thereof, calculated as tenofovir alafenamide free base;

(b) 200 mg emtricitabine, or a pharmaceutically acceptable salt thereof, calculated as emtricitabine free base;

(c) excipients selected from:

(i) microcrystalline cellulose or lactose;

(ii) croscarmellose sodium or crospovidone; and

(iii) magnesium stearate; and

(d) coating;

wherein the tablet contains only two active pharmaceutical ingredients: tenofovir alafenamide, or a pharmaceutically acceptable salt thereof, and emtricitabine, or a pharmaceutically acceptable salt thereof; and

wherein the tablet has a total weight of less than 600 mg.

2 . The tablet according to claim 1 , wherein the tablet has a total weight of less than 500 mg.

3 . The tablet according to claim 2 , wherein the tablet has a total weight of more than 350 mg.

4 . The tablet according to claim 3 , wherein the tablet contains a pharmaceutically acceptable salt of tenofovir alafenamide, and the pharmaceutically acceptable salt is a fumarate salt.

5 . The tablet according to claim 4 , wherein less than about 250 mg of the tablet is the excipients.

6 . The tablet according to claim 5 , wherein the tablet contains less than 200 mg of microcrystalline cellulose or less than 200 mg of lactose.

7 . The tablet according to claim 4 , wherein:

less than about 40% by weight of the tablet is microcrystalline cellulose or lactose;

less than about 20% by weight of the tablet is croscarmellose sodium or crospovidone; and

about 0.5 w/w % to about 5 w/w % of the tablet is magnesium stearate.

8 . The tablet according to claim 4 , wherein less than 250 mg of the tablet is the excipients.

9 . The tablet according to claim 8 , wherein more than 100 mg of the tablet is the excipients.

10 . The tablet according to claim 9 , wherein the tablet contains less than 200 mg of microcrystalline cellulose or less than 200 mg of lactose.

11 . The tablet according to claim 4 , wherein:

less than 40% by weight of the tablet is microcrystalline cellulose or lactose;

less than 20% by weight of the tablet is croscarmellose sodium or crospovidone; and

0.5 w/w % to 5 w/w % of the tablet is magnesium stearate.

12 . A tablet, consisting of:

(a) a fumarate salt of tenofovir alafenamide, equivalent to 25 mg tenofovir alafenamide free base;

(b) 200 mg emtricitabine;

(c) excipients selected from:

(i) microcrystalline cellulose or lactose;

(ii) croscarmellose sodium or crospovidone; and

(iii) magnesium stearate; and

(d) a coating;

wherein the tablet contains only two active pharmaceutical ingredients: the fumarate salt of tenofovir alafenamide, and emtricitabine; and

wherein the tablet has a total weight between 300 mg and 500 mg.

13 . The tablet according to claim 12 , wherein more than 100 mg of the tablet is the excipients.

14 . The tablet according to claim 12 , wherein less than about 250 mg of the tablet is the excipients.

15 . The tablet according to claim 14 , wherein more than 100 mg of the tablet is the excipients.

16 . The tablet according to claim 14 , wherein the tablet contains less than 200 mg of microcrystalline cellulose or less than 200 mg of lactose.

17 . The tablet according to claim 12 , wherein:

less than about 40% by weight of the tablet is microcrystalline cellulose or lactose;

less than about 20% by weight of the tablet is croscarmellose sodium or crospovidone; and

about 0.5 w/w % to about 5 w/w % of the tablet is magnesium stearate.

18 . The tablet according to claim 12 , wherein less than 250 mg of the tablet is the excipients.

19 . The tablet according to claim 18 , wherein more than 100 mg of the tablet is the excipients.

20 . The tablet according to claim 18 , wherein the tablet contains less than 200 mg of microcrystalline cellulose or less than 200 mg of lactose.

21 . A tablet, consisting of:

(a) 25 mg tenofovir alafenamide, or a fumarate salt thereof, calculated as tenofovir alafenamide free base;

(b) 200 mg emtricitabine, or a pharmaceutically acceptable salt thereof, calculated as emtricitabine free base;

(c) excipients selected from:

(i) microcrystalline cellulose, lactose, mannitol, or dibasic calcium phosphate;

(ii) croscarmellose sodium or crospovidone; and

(iii) magnesium stearate; and

(d) a coating;

wherein the tablet contains only two active pharmaceutical ingredients: tenofovir alafenamide, or a fumarate salt thereof, and emtricitabine, or a pharmaceutically acceptable salt thereof; and

wherein the tablet has a total weight of about 450 mg.

22 . The tablet according to claim 21 , wherein the tenofovir alafenamide, or a fumarate salt thereof, is a fumarate salt of tenofovir alafenamide.

23 . The tablet according to claim 22 , wherein the excipients are selected from:

(i) microcrystalline cellulose or lactose;

(ii) croscarmellose sodium or crospovidone; and

(iii) magnesium stearate.

24 . The tablet according to claim 23 , wherein less than about 250 mg of the tablet is the excipients.

25 . The tablet according to claim 23 , wherein the tablet contains less than 200 mg of microcrystalline cellulose or less than 200 mg of lactose.

26 . The tablet according to claim 23 , wherein:

less than about 40% by weight of the tablet is microcrystalline cellulose or lactose;

less than about 20% by weight of the tablet is croscarmellose sodium or crospovidone; and

about 0.5 w/w % to about 5 w/w % of the tablet is magnesium stearate.

27 . A tablet, consisting of:

(a) a fumarate salt of tenofovir alafenamide, equivalent to 25 mg tenofovir alafenamide free base;

(b) 200 mg emtricitabine, or a pharmaceutically acceptable salt thereof, calculated as emtricitabine free base;

(c) excipients selected from:

(i) microcrystalline cellulose or lactose;

(ii) croscarmellose sodium or crospovidone; and

(iii) magnesium stearate; and

(d) a coating;

wherein the tablet contains only two active pharmaceutical ingredients: the fumarate salt of tenofovir alafenamide, and emtricitabine, or a pharmaceutically acceptable salt thereof; and

wherein the tablet has a total weight of 350 mg±50 mg.

28 . The tablet according to claim 27 , wherein the fumarate salt is tenofovir alafenamide hemifumarate.

29 . The tablet according to claim 28 , wherein:

less than about 40% by weight of the tablet is microcrystalline cellulose or lactose;

less than about 20% by weight of the tablet is croscarmellose sodium or crospovidone; and

about 0.5 w/w % to about 5 w/w % of the tablet is magnesium stearate.