Catalog No.S1276 Synonyms: CD-271
Molecular Weight(MW): 412.52
Adapalene is a dual RAR and RXR agonist, used in the treatment of acne.
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|Description||Adapalene is a dual RAR and RXR agonist, used in the treatment of acne.|
Adapalene binds to retinoic acid receptors found predominantly in the terminal differentiation zone of epidermis and is more active than tretinoin in modulating cellular differentiation. Adapalene shows greatest affinity for the subtype PARγ, found predominantly in the epidermis. Adapalene is more active than indomethacin, betamethasone valerate, tretinoin, isotretinoin or etretinate in inhibiting lipoxygease activity, but it has little activity against cyclo-oxygenase.  Adapalene time- and dose-dependently suppresses DNA synthesis and induces apoptosis in Colon carcinoma cell lines CC-531, HT-29 and LOVO as well as human foreskin fibroblasts. Adapalene shows significantly more effective antiproliferative and proapoptotic effects than 9-cis-retinoic acid (CRA), showing remarkable effects even at 10 μM. Adapalene disrupts DeltaPsi(m) and induces caspase-3 activity in responsive tumor cells. 
|In vivo||Adapalene produces a dose-related reduction in the number of epidermal comedones and an increase in comedo profile and epidermal thickness in the rhino mice.  Adapalene results in a decreased expression of TLR-2 and IL-10 in explants of normal skin and explants of acne. Adapalene can modulate the epidermal immune system by increasing the CD1d expression and by decreasing the IL-10 expression by keratinocytes, and these modulations can increase the interactions between dendritic cells and T lymphocytes and could strengthen the antimicrobial activity against Propionibacterium acnes. |
|In vitro||DMSO||8 mg/mL (19.39 mM)|
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Clinical Trial Information
|NCT Number||Recruitment||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT02932267||Not yet recruiting||Acne Vulgaris||Galderma||December 2016||Phase 3|
|NCT02899000||Active, not recruiting||Acne Vulgaris||Galderma Laboratories, L.P.||July 2016||Phase 4|
|NCT02735421||Active, not recruiting||Acne Vulgaris|Atrophic Acne Scars||Galderma||May 2016||Phase 4|
|NCT02721173||Completed||Acne Vulgaris||All India Institute of Medical Sciences, Bhubaneswar||April 2016||Phase 4|
|NCT02755545||Active, not recruiting||Acne||Galderma Laboratories, L.P.||April 2016||Phase 4|
|NCT02651220||Completed||Acne||Actavis Inc.||November 2015||Phase 3|
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