COMPOUNDS, COMPOSITIONS, KITS AND METHODS OF USE TO ORALLY AND TOPICALLY TREAT ACNE AND OTHER SKIN CONDITIONS BY ADMINISTERING A 19-NOR CONTAINING VITAMIN D ANALOG WITH OR WITHOUTA RETINOID

摘要

Oral and topical pharmaceutical compositions, kits and methods of treatment thereof for treating various skin disorder including acne, psoriasis, ichthyosis, photoaging, photodamaged skin, and, skin cancer. Exemplary vitamin D analogs as active pharmaceutical ingredients include 2-methylene-19-nor-20(S)-l.alpha.-hydroxy-bishomopregnacalciferol, 19-nor- 26,27-dimethylene-20(S)-2-methylene-l.alpha.,25-dihydroxyvitamin D3, 2-methylene-l.alpha.,25- dihydroxy-( 17E)- 17(20)-dehydro- 19-nor-vitamin D3, 2-methylene- 19-nor-(24R)- 1 .alpha.,25- dihydroxyvitamin D2, 2-methylene-(20R,25S)-19,26-dinor-l.alpha.,25-dihydroxyvitamin D3, 2- methylene- 19-nor- 1 .alpha.-hydroxy-pregnacalciferol, 1 .alpha.-hydroxy-2-methylene- 19-nor- homopregnacalciferol, (20R)- 1 .alpha.-hydroxy-2-methylene- 19-nor-bishomopregnacalciferol, 2- methylene- 19-nor-(20S)- 1 .alpha.-hydroxy-trishomopregnacalciferol, 2-methylene-23,23-difluoro- 1 .alpha.-hydroxy- 19-nor-bishomopregnacalciferol, 2-methylene-(20S)-23,23 -difluoro- 1 .alpha.-hydroxy- 19-nor-bishomopregnancalciferol, (2 -(3 'hydroxypropyl- 1 ',2 ' -idene)- 19,23,24-trinor-(20S)- l.alpha.-hydroxyvitamin D3, 2-methylene- 18, 19-dinor-(20S)-l.alpha.,25-dihydroxyvitamin D3, a stereoisomer thereof, a prodrug thereof in oral compositions, a salt thereof, and/or a solute thereof. Compounds that activate retinoic acid receptors, such as retinoyls and retinoyl esters, include 13-cw-retmoic acid, all-trafls-retinoic acid, (2E,4E,6Z,8E)-3,7-dimethyl-9- (2,6,6-trimethyl-l-cyclohexeneyl)nona-2,4,6,8-tetraenoic acid, 9-(4-methoxy-2,3,6-trimethyl- phenyl)-3,7-dimethyl-nona-2,4,6, 8-tetraenoic acid, 6- [3 -( 1 -adamantyl)-4-methox yphenyl] -2- napthoic acid, 4-[l-(3,5,5,8,8-pentamethyl-tetralin-2-yl)ethenyl]benzoic acid, retinobenzoic acid, ethyl 6-[2-(4,4-dimethylthiochroman-6-yl)ethynyl]pyridine-3-carboxylate, retinoyl t- butyrate, retinoyl pinacol, retinoyl cholesterol, an isomer thereof, a prodrug thereof for oral compositions, an ester thereof, a salt thereof, and/or, a solute thereof. Combinations of such active ingredients demonstrate synergistic efficacy.