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Alitretinoin

(British Approved Name, US Adopted Name, rINN)

Drug Nomenclature

International Nonproprietary Names (INNs) in main languages (French, Latin, Russian, and Spanish):

AlitretinoinSynonyms: 9-cis-Retinoic Acid; AGN-192013; ALRT-1057; Alitretinoína; Alitretinoiini; Alitretinoin; Alitretinoinum; BAL-4079; LG-100057; LGD-1057; NSC-659772
BAN: Alitretinoin
USAN: Alitretinoin
INN: Alitretinoin [rINN (en)]
INN: Alitretinoína [rINN (es)]
INN: Alitrétinoïne [rINN (fr)]
INN: Alitretinoinum [rINN (la)]
INN: Алитретиноин [rINN (ru)]
Chemical name: (2E,4E,6Z,8E)-3,7-Dimethyl-9-(2,6,6-trimethyl-1-cyclohexen-1-yl)-2,4,6,8-nonatetraenoic acid
Molecular formula: C20H28O2 =300.4
CAS: 5300-03-8
ATC code: L01XX22

Adverse Effects and Precautions

Local skin toxicity may occur with topical application of alitretinoin, in particular erythema and oedema, and in some patients this may be dose-limiting. Pain, paraesthesia, rashes, pruritus, exfoliative dermatitis, and other skin disorders may also occur locally. Lymphadenopathy, phlebitis, cellulitis, and bacterial infections have been reported. Alitretinoin may have a weak photosensitising effect, and patients should minimise exposure of treated areas to sunlight or other ultraviolet light during therapy.

Interactions

Use of products containing diethyltoluamide is not recommended during alitretinoin therapy, as animal studies indicate an increase in diethyltoluamide toxicity with concurrent use.

Pharmacokinetics

Systemic absorption of topical alitretinoin is not considered to be extensive. In-vivo studies of oral doses indicate that alitretinoin is metabolised to 4-oxo-9-ds-retinoic acid.

Uses and Administration

Alitretinoin is a retinoid related to tretinoin. It is used topically, as a 0.1% gel, in the management of cutaneous lesions in patients with AIDS-related Kaposi’s sarcoma. It is applied directly to the lesions twice daily, increasing to up to 4 times daily if tolerated. Doses should be increased at intervals of at least 2 weeks. If local toxicity occurs, application frequency should be reduced, or treatment temporarily stopped, until the symptoms subside. EU licensed product information states that if no response is seen after 12 weeks, therapy should be stopped; however, US licensed product information states that some patients have required over 14 weeks to respond. Treatment may be continued as long as the patient responds. Oral formulations of alitretinoin are under investigation for the treatment of chronic hand dermatitis refractory to topical corticosteroids.

Single-ingredient Preparations

The symbol ¤ denotes a preparation which is discontinued or no longer actively marketed.

Canada: Panretin¤; France: Panretin; Greece: Panretin; United States: Panretin

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