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 pharmaceutical composition, suitable for topical skin application to a human patient with a skin disorder, 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.
2. The composition according to claim 1 , wherein the composition is suitable for application to the patient's skin for up to 84 consecutive days.
3. The composition according to claim 1 , wherein the skin disorder is an autoimmune skin disorder.
4. The composition according to claim 1 , wherein the skin disorder is associated with JAK1 and/or JAK2.
5. The composition 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.
6. The composition according to claim 1 , wherein the skin disorder is atopic dermatitis.
7. The composition 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.
8. A pharmaceutical composition, suitable for topical skin application to a human patient with a skin disorder, 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.
9. The composition according to claim 8 , wherein the composition is suitable for application to the patient's skin for up to 84 consecutive days.
10. The composition according to claim 8 , wherein the skin disorder is an autoimmune skin disorder.
11. The composition according to claim 8 , wherein the skin disorder is associated with JAK1 and/or JAK2.
12. The composition according to claim 8 , wherein the skin disorder is chosen from pemphigus vulgaris (PV), bullous pemphigoid (BP), psoriasis, psoriasis vulgaris, atopic dermatitis, and combinations thereof.
13. The composition according to claim 8 , wherein the skin disorder is atopic dermatitis.
14. The composition according to claim 8 , 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.
15. A pharmaceutical composition, suitable for topical skin application to a human patient with a skin disorder, 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.
16. The composition according to claim 15 , wherein the composition is suitable for application to the patient's skin for up to 84 consecutive days.
17. The composition according to claim 15 , wherein the skin disorder is an autoimmune skin disorder.
18. The composition according to claim 15 , wherein the skin disorder is associated with JAK1 and/or JAK2.
19. The composition according to claim 15 , wherein the skin disorder is chosen from pemphigus vulgaris (PV), bullous pemphigoid (BP), psoriasis, psoriasis vulgaris, atopic dermatitis, and combinations thereof.
20. The composition according to claim 15 , wherein the skin disorder is atopic dermatitis.
21. The composition according to claim 15 , 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 pharmaceutical composition, suitable for topical skin application to a human patient with a skin disorder, 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.
23. The composition according to claim 22 , wherein the composition is suitable for application to the patient's skin for up to 84 consecutive days.
24. The composition according to claim 22 , wherein the skin disorder is an autoimmune skin disorder.
25. The composition according to claim 22 , wherein the skin disorder is associated with JAK1 and/or JAK2.
26. The composition 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.
27. The composition according to claim 22 , wherein the skin disorder is atopic dermatitis.
28. The composition 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.