Topical formulation for a JAK inhibitor
This invention relates to pharmaceutical formulations for topical skin application comprising (R)-3-cyclopentyl-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]propanenitrile, or a pharmaceutically acceptable salt thereof, and use in the treatment of skin disorders.
1. A method of treating a skin disorder in a human patient in need thereof comprising:
applying to the patient's skin a pharmaceutically composition comprising: 1) a therapeutic agent present in an amount ranging from about 0.5% to about 1.5% by weight of the composition, wherein the therapeutic agent is (R)-3-cyclopentyl-3-[4 (7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]propanenitrile or a pharmaceutically acceptable salt thereof, and (2) a means for effecting skin permeation of (R)-3-cyclopentyl-3-[4 (7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]propanenitrile to the patient, wherein the treating step is one or more of (a) inhibiting the skin disorder and (b) ameliorating the skin disorder.
2. The method according to claim 1 , wherein the applying step comprises application up to 84 consecutive days to the patient's skin.
3. The method according to claim 1 , wherein the applying step is repeatable.
4. The method according to claim 1 , wherein the applying step comprises daily application to the patient's skin.
5. The method according to claim 1 , wherein the skin disorder is an autoimmune skin disorder.
6. The method according to claim 1 , wherein the skin disorder is associated with JAK1 and/or JAK2.
7. The method according to claim 1 , wherein the skin disorder is chosen from pemphigus vulgaris (PV), bullous pemphigoid (BP), psoriasis, psoriasis vulgaris, atopic dermatitis, and combinations thereof.
8. The method according to claim 1 , wherein the skin disorder is atopic dermatitis.
9. The method according to claim 1 , wherein the therapeutic agent is (R)-3-cyclopentyl-3-[4 (7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]propanenitrile phosphoric acid salt.
10. A method of treating a skin disorder in a human patient in need thereof comprising:
applying to the patient's skin a pharmaceutical composition comprising: (1) a therapeutic agent present in an amount of about 0.5% by weight of the composition, wherein the therapeutic agent is (R)-3-cyclopentyl-3-[4 (7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]propanenitrile or a pharmaceutically acceptable salt thereof, and (2) a means for effecting skin permeation of (R)-3-cyclopentyl-3-[4 (7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]propanenitrile to the patient, wherein the treating step is one or more of (a) inhibiting the skin disorder and (b) ameliorating the skin disorder.
11. The method according to claim 10 , wherein the skin disorder is an autoimmune skin disorder.
12. The method according to claim 10 , wherein the skin disorder is associated with JAK1 and/or JAK2.
13. The method according to claim 10 , wherein the skin disorder is chosen from pemphigus vulgaris (PV), bullous pemphigoid (BP), psoriasis, psoriasis vulgaris, atopic dermatitis, and combinations thereof.
14. The method according to claim 10 , wherein the skin disorder is atopic dermatitis.
15. The method according to claim 10 , wherein the therapeutic agent is (R)-3-cyclopentyl-3-[4 (7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]propanenitrile phosphoric acid salt.
16. A method of treating a skin disorder in a human patient in need thereof comprising:
applying to the patient's skin a pharmaceutical composition comprising: (1) a therapeutic agent present in an amount of about 1.0% by weight of the composition, wherein the therapeutic agent is (R)-3-cyclopentyl-3-[4 (7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]propanenitrile or a pharmaceutically acceptable salt thereof, and (2) a means for effecting skin permeation of (R)-3-cyclopentyl-3-[4 (7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]propanenitrile to the patient, wherein the treating step is one or more of (a) inhibiting the skin disorder and (b) ameliorating the skin disorder.
17. The method according to claim 16 , wherein the skin disorder is an autoimmune skin disorder.
18. The method according to claim 16 , wherein the skin disorder is associated with JAK1 and/or JAK2.
19. The method according to claim 16 , wherein the skin disorder is chosen from pemphigus vulgaris (PV), bullous pemphigoid (BP), psoriasis, psoriasis vulgaris, atopic dermatitis, and combinations thereof.
20. The method according to claim 16 , wherein the skin disorder is atopic dermatitis.
21. The method according to claim 16 , wherein the therapeutic agent is (R)-3-cyclopentyl-3-[4 (7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]propanenitrile phosphoric acid salt.
22. A method of treating a skin disorder in a human patient in need thereof comprising:
applying to the patient's skin a pharmaceutical composition comprising: (1) a therapeutic agent present in an amount of about 1.5% by weight of the composition, wherein the therapeutic agent is (R)-3-cyclopentyl-3-[4 (7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]propanenitrile or a pharmaceutically acceptable salt thereof, and (2) a means for effecting skin permeation of (R)-3-cyclopentyl-3-[4 (7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]propanenitrile to the patient, wherein the treating step is one or more of (a) inhibiting the skin disorder and (b) ameliorating the skin disorder.
23. The method according to claim 22 , wherein the skin disorder is an autoimmune skin disorder.
24. The method according to claim 22 , wherein the skin disorder is associated with JAK1/JAK2.
25. The method according to claim 22 , wherein the skin disorder is chosen from pemphigus vulgaris (PV), bullous pemphigoid (BP), psoriasis, psoriasis vulgaris, atopic dermatitis, and combinations thereof.
26. The method according to claim 22 , wherein the skin disorder is atopic dermatitis.
27. The method according to claim 22 , wherein the therapeutic agent is (R)-3-cyclopentyl-3-[4 (7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]propanenitrile phosphoric acid salt.