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出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2015/05/28 20:05:57」(JST)

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Adapalene is a second-generation topical retinoid primarily used in the treatment of mild-moderate acne, and is also used off-label to treat keratosis pilaris as well as other skin conditions.^[1] It is effective against acne conditions where comedones are predominant.

History

Adapalene is a research product of Galderma Laboratories, France.^{[citation needed]} Adapalene was approved in 1996 by the U.S. Food and Drug Administration (FDA) for use in the treatment of acne.^{[citation needed]} Generics are now available in US and India

Mechanism of action

Unlike tretinoin, adapalene inhibits keratinocyte differentiation. This inhibition of keratinocyte differentiation and proliferation is responsible for adapalene’s comedolytic effect. It has both exfoliating and anti-inflammatory effects. In an in vivo study, adapalene’s ability to reduce comedo formation was demonstrated by a 50–60% reduction in comedo counts compared with vehicle.

Available forms

Tube of generic adapalene

In the United States, adapalene is available under the brand name Differin in three different preparations: 0.1% cream, 0.1% gel, and 0.3% gel.^[2] The 0.1% gel is available as a generic made by Teva.^[3]^[4] It is also available combined with benzoyl peroxide under the brand name Epiduo.^[5] In Europe, only the 0.1% cream and 0.1% gel are available. Adapalene is currently marketed by Galderma under the trade names Differin in some countries, and Adaferin in India.^[6] It is mostly available in 0.1% w /w gel form.

Pharmacology

Drug interactions

Adapalene has been shown to enhance the efficacy of topical clindamycin, although adverse effects are also increased.^[7] Application of adapalene gel to the skin 3–5 minutes before application of clindamycin enhances penetration of clindamycin into the skin, which may enhance the overall efficacy of the treatment as compared to clindamycin alone.^[8]

Unlike tretinoin (Retin-A), adapalene has also been shown to retain its efficacy when applied at the same time as benzoyl peroxide due to its more stable chemical structure.^[9]

Pharmacokinetics

Absorption of adapalene through the skin is low. A study with six acne patients treated once daily for five days with two grams of adapalene cream applied to 1000 cm² of skin found no quantifiable amounts, or less than 0.35 ng/mL of the drug, in the patients' blood plasma.^[10]

References

^ Rolewski S (2003). "Clinical review: topical retinoids". Dermatol Nurs 15 (5): 447–50, 459–65. PMID 14619325.
^ About Differin
^ "Teva Introduces Adapalene Gel, 0.1%". PharmQD. 4 June 2010. Retrieved 30 Aug 2011.
^ Webber, Keith (2 June 2010). "FDA Approval Letter" (PDF). Department of Health and Human Services. Retrieved 30 August 2011.
^ http://www.webmd.com/news/20090106/fda-oks-new-acne-gel-epiduo
^ http://www.drugsupdate.com/brand/generic/Adapalene/7099/none/2
^ Wolf JE, Kaplan D, Kraus SJ et al. (2003). "Efficacy and tolerability of combined topical treatment of acne vulgaris with adapalene and clindamycin: a multicenter, randomized, investigator-blinded study". J Am Acad Dermatol 49 (3 Suppl): S211–7. doi:10.1067/S0190-9622(03)01152-6. PMID 12963897.
^ Jain GK, Ahmed FJ (2007). "Adapalene pretreatment increases follicular penetration of clindamycin: in vitro and in vivo studies". Indian J Dermatol Venereol Leprol 73 (5): 326–9. doi:10.4103/0378-6323.34010. PMID 17921613.
^ Martin B, Meunier C, Montels D, Watts O (October 1998). "Chemical stability of adapalene and tretinoin when combined with benzoyl peroxide in presence and in absence of visible light and ultraviolet radiation". Br J Dermatol. 139 Suppl 52: 8–11. doi:10.1046/j.1365-2133.1998.1390s2008.x. PMID 9990414.
^ "DIFFERIN® (adapalene) Cream, 0.1% Label" (PDF). FDA. May 25, 2000. Retrieved 4 Oct 2011.

External links

Adapalene General Information, Patient Information, Contraindications and Interactions
Epiduo Prescribing Information

UpToDate Contents

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1. 尋常性ざ瘡の治療 treatment of acne vulgaris
2. 口囲（口周囲の）皮膚炎 perioral periorificial dermatitis
3. ダリエ病 darier disease
4. 光線角化症の治療 treatment of actinic keratosis
5. 尋常性ざ瘡のための光治療、補助化学療法、およびその他の治療法 light based adjunctive and other therapies for acne vulgaris

English Journal

Adapalene inhibits the activity of cyclin-dependent kinase 2 in colorectal carcinoma.

Shi XN1, Li H2, Yao H3, Liu X1, Li L1, Leung KS2, Kung HF1, Lin MC1.
Molecular medicine reports.Mol Med Rep.2015 Sep 10. doi: 10.3892/mmr.2015.4310. [Epub ahead of print]
Cyclin-dependent kinase 2 (CDK2) has been reported to be overexpressed in human colorectal cancer; it is responsible for the G1‑to‑S‑phase transition in the cell cycle and its deregulation is a hallmark of cancer. The present study was the first to use idock, a free and open‑source protein�
PMID 26398439

A double-blinded, randomized, vehicle-controlled study to access skin tolerability and efficacy of an anti-inflammatory moisturizer in treatment of acne with 0.1% adapalene gel.

Chularojanamontri L1, Tuchinda P, Kulthanan K, Varothai S, Winayanuwattikun W.
The Journal of dermatological treatment.J Dermatolog Treat.2015 Sep 2:1-6. [Epub ahead of print]
INTRODUCTION: Topical retinoids are considered to be the first-line agents and maintenance therapy of acne; however, irritation side effects are major concern issues. Noncomedogenic moisturizers are sometimes added to relieve cutaneous irritations. This study aimed to compare tolerability and effica
PMID 26293170

Allergic contact dermatitis caused by adapalene.

Numata T1, Jo R1, Kobayashi Y1, Tsuboi R1, Okubo Y1.
Contact dermatitis.Contact Dermatitis.2015 Sep;73(3):187-8. doi: 10.1111/cod.12410. Epub 2015 May 11.
PMID 25960068

Japanese Journal

アダパレン外用が奏効したFavre-Racouchot症候群の2例 (特集毛包・脂腺系疾患 : 最近の話題)

皮膚科の臨床 56(3), 327-330, 2014-03
NAID 40020024415

EGFR-TKIによるざ瘡様皮疹に対しアダパレンが有効であった2例

肺癌 54(7), 978-982, 2014
NAID 130004880437

臨床統計治療ガイドライン策定とアダパレン登場による皮膚科診療施設での痤瘡治療実態の変化 : 2007年と2010年との比較

臨床皮膚科 67(4), 367-374, 2013-04
NAID 40019656262

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「アダパレン」

Adapalene
Systematic (IUPAC) name
	6-[3-(1-adamantyl)-4-methoxy-phenyl] naphthalene-2-carboxylic acid
Clinical data
Trade names	Differin, Teva, Pimpal, Gallet, Adelene, Adeferin
AHFS/Drugs.com	monograph
MedlinePlus	a604001
Licence data	US FDA:link
Pregnancy; category	AU: D; US: C (Risk not ruled out);
Legal status	AU: Prescription Only (S4); CA: ℞-only; UK: Prescription-only (POM); US: ℞-only;
Routes of; administration	Topical
Pharmacokinetic data
Bioavailability	Very low
Excretion	Biliary
Identifiers
CAS Registry Number	106685-40-9
ATC code	D10AD03
PubChem	CID 60164
DrugBank	DB00210
ChemSpider	54244
UNII	1L4806J2QF
KEGG	D01112
ChEBI	CHEBI:31174
ChEMBL	CHEMBL1265
Chemical data
Formula	C28H28O3
Molecular mass	412.52 g/mol
	SMILES O=C(O)c2ccc1cc(ccc1c2)c3cc(c(OC)cc3)C46CC5CC(CC(C4)C5)C6;
	InChI InChI=1S/C28H28O3/c1-31-26-7-6-23(21-2-3-22-12-24(27(29)30)5-4-20(22)11-21)13-25(26)28-14-17-8-18(15-28)10-19(9-17)16-28/h2-7,11-13,17-19H,8-10,14-16H2,1H3,(H,29,30) ; Key:LZCDAPDGXCYOEH-UHFFFAOYSA-N ;
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英: adapalene
商: ディフェリン
関: その他の外皮用薬

[1] Rolewski S (2003). "Clinical review: topical retinoids". Dermatol Nurs 15 (5): 447–50, 459–65. PMID 14619325.

[2] About Differin

[3] "Teva Introduces Adapalene Gel, 0.1%". PharmQD. 4 June 2010. Retrieved 30 Aug 2011.

[4] Webber, Keith (2 June 2010). "FDA Approval Letter" (PDF). Department of Health and Human Services. Retrieved 30 August 2011.

[5] ttp://www.webmd.com/news/20090106/fda-oks-new-acne-gel-epiduo

[6] ttp://www.drugsupdate.com/brand/generic/Adapalene/7099/none/2

[Wolf-7] Wolf JE, Kaplan D, Kraus SJ et al. (2003). "Efficacy and tolerability of combined topical treatment of acne vulgaris with adapalene and clindamycin: a multicenter, randomized, investigator-blinded study". J Am Acad Dermatol 49 (3 Suppl): S211–7. doi:10.1067/S0190-9622(03)01152-6. PMID 12963897.

[Jain-8] Jain GK, Ahmed FJ (2007). "Adapalene pretreatment increases follicular penetration of clindamycin: in vitro and in vivo studies". Indian J Dermatol Venereol Leprol 73 (5): 326–9. doi:10.4103/0378-6323.34010. PMID 17921613.

[9] Martin B, Meunier C, Montels D, Watts O (October 1998). "Chemical stability of adapalene and tretinoin when combined with benzoyl peroxide in presence and in absence of visible light and ultraviolet radiation". Br J Dermatol. 139 Suppl 52: 8–11. doi:10.1046/j.1365-2133.1998.1390s2008.x. PMID 9990414.

[productLabel-10] "DIFFERIN® (adapalene) Cream, 0.1% Label" (PDF). FDA. May 25, 2000. Retrieved 4 Oct 2011.

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