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Brand name: Panretin
Drug class: Skin and Mucous Membrane Agents, Miscellaneous
VA class: DE600
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
CAS number: 5300-03-8

Medically reviewed by on Jan 24, 2022. Written by ASHP.


A vitamin A derivative; naturally occurring endogenous retinoid with topical antineoplastic activity.

Uses for Alitretinoin

AIDS-related Kaposi’s Sarcoma

Treatment of cutaneous lesions associated with AIDS-related Kaposi’s sarcoma.

Not recommended for treatment of systemic AIDS-related Kaposi’s sarcoma, characterized by ≥10 new lesions in the prior month, symptomatic lymphedema, symptomatic pulmonary Kaposi’s sarcoma, or symptomatic visceral disease.

No clinical experience to date in patients receiving systemic therapy for Kaposi’s sarcoma.

Alitretinoin Dosage and Administration


Topical Administration

Apply topically to skin.

Wait 20 minutes after bathing or showering before applying gel; avoid use of occlusive dressings or wrappings.

Avoid contact with healthy skin or mucous membranes (e.g., eyes, nostrils, mouth, lips, vagina, tip of penis, rectum, anus); irritation may occur.

Allow gel to dry for 3–5 minutes before covering treated area with clothing.

If possible, do not bathe, shower, or swim for at least 3 hours after application.

If application-site toxicity occurs, reduce application frequency.

If severe irritation occurs, discontinue temporarily until manifestations subside.



AIDS-related Kaposi’s Sarcoma

Initially, apply twice daily in sufficient amounts (to cover only affected areas). May increase application frequency gradually to 3 and then 4 times daily, according to individual lesion tolerance.

In some patients, appreciable response occurred only after 14 weeks of therapy.

Continue therapy as long as the patient derives benefit (has been applied for up to 175 weeks in clinical trials).

Cautions for Alitretinoin


  • Known hypersensitivity to retinoids or any ingredient in the formulation.



Fetal/Neonatal Morbidity and Mortality

May cause fetal harm; teratogenicity and embryotoxicity demonstrated in animals receiving oral alitretinoin. No reproduction studies in animals with topical alitretinoin.

No adequate and well-controlled studies in humans. Avoid pregnancy during therapy. If used during pregnancy, apprise of potential hazard to the fetus.

Sensitivity Reactions


Retinoids associated with photosensitivity; in vitro data indicate alitretinoin may have weak photosensitizing effect.

Minimize exposure of treated areas to natural or artificial (e.g., sunlamps) sunlight.

Major Toxicities

Dermatologic Effects

Possible severe local skin reactions (e.g., intense erythema, edema, vesiculation). Patients with cutaneous T-cell lymphoma exhibit less tolerance to these effects than those with Kaposi’s sarcoma.

Specific Populations


Category D. (See Fetal/Neonatal Morbidity and Mortality under Cautions.)


Not known whether alitretinoin or its metabolites are distributed into milk; discontinue nursing due to risk in nursing infants.

Pediatric Use

Safety and efficacy not established in children <18 years of age.

Geriatric Use

Insufficient clinical experience in patients ≥65 years of age to determine whether they respond differently than younger adults.

Common Adverse Effects

Rash, pruritus, exfoliative dermatitis, skin disorders (excoriation, cracking, scabbing, crusting, drainage, eschar, fissure, oozing ), pain, paresthesia, edema.

Interactions for Alitretinoin

Metabolized by CYP2C9, CYP3A4, CYP1A1, and CYP1A2.

No data available on interactions between topical alitretinoin and systemically administered drugs for Kaposi’s sarcoma.

Specific Drugs




Antifungals, azoles

No clinical evidence of interactions during concomitant use

Unknown effect on steady-state concentrations of azole antifungals

Antiretroviral agents (including protease inhibitors)

No clinical evidence of interactions during concomitant use

Unknown effect on steady-state concentrations of antiretroviral agents

Diethyltoluamide (DEET)

Increased DEET toxicity observed in animals

Avoid concomitant use

Macrolide antibiotics

No clinical evidence of interactions during concomitant use

Unknown effect on steady-state concentrations of macrolide antibiotics

Alitretinoin Pharmacokinetics



Not substantially absorbed systemically following topical application.

Following repeated, multiple-daily-dose topical applications of alitretinoin (9-cis-retinoic acid) in patients with cutaneous lesions associated with Kaposi’s sarcoma, plasma concentrations of 9-cis-retinoic acid were similar to those of naturally occurring 9-cis-retinoic acid found in healthy untreated patients.



Not known whether alitretinoin or its metabolites are distributed into milk.



Alitretinoin metabolized to 4-hydroxy-9-cis-retinoic acid and 4-oxo-9-cis-retinoic acid by CYP2C9, CYP3A4, CYP1A1, and CYP1A2 in vitro; major circulating metabolite in vivo following oral alitretinoin is 4-oxo-9-cis-retinoic acid.

Elimination Route

Principally by metabolism; no unchanged drug excreted in urine.


1.3–2.4 hours following oral administration.





25°C (may be exposed to 15–30°C).


  • Binds to and activates both intracellular retinoic acid receptors (RAR) (e.g., RARα, RARβ, RARγ) and retinoid X receptors (RXR) (e.g., RXRα, RXRβ, RXRγ) that appear to enhance gene transcription.

  • Exact mechanism of action in Kaposi’s sarcoma not fully elucidated; appears to affect expression of genes that inhibit cell proliferation, induce cell differentiation, and trigger apoptosis in both healthy and cancer cells.

  • In vitro, alitretinoin appears to inhibit Kaposi’s sarcoma cell growth.

Advice to Patients

  • Provide patients with a copy of manufacturer’s patient information.

  • Describe risk of photosensitivity and associated precautions.

  • Importance of women informing clinicians if they are or plan to become pregnant or plan to breast-feed. Necessity of advising women to avoid pregnancy during therapy.

  • Importance of informing clinicians of existing or contemplated concomitant therapy, including prescription and OTC drugs, as well as any concomitant illnesses.

  • Importance of informing patients of other important precautionary information. (See Cautions.)


Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details.

Please refer to the ASHP Drug Shortages Resource Center for information on shortages of one or more of these preparations.



Dosage Forms


Brand Names




0.1% w/w

Panretin (with dehydrated alcohol)


AHFS DI Essentials™. © Copyright 2022, Selected Revisions February 1, 2005. American Society of Health-System Pharmacists, Inc., 4500 East-West Highway, Suite 900, Bethesda, Maryland 20814.

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