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Alitretinoin (Topical)

Medically reviewed by Drugs.com. Last updated on Jul 1, 2020.

Pronunciation

(a li TRET i noyn)

Index Terms

  • 9-cis-retinoic acid

Dosage Forms

Excipient information presented when available (limited, particularly for generics); consult specific product labeling.

Gel, External:

Panretin: 0.1% (60 g)

Brand Names: U.S.

  • Panretin

Pharmacologic Category

  • Antineoplastic Agent, Retinoic Acid Derivative

Pharmacology

Alitretinoin is a naturally occurring endogenous retinoid that binds to and activates intracellular retinoid receptors (RAR and RXR subtypes); this results in altered expression of the genes controlling cellular differentiation and proliferation in normal and neoplastic cells, inhibiting the growth of Kaposi sarcoma

Absorption

Not extensive

Use: Labeled Indications

Kaposi sarcoma: Topical treatment of cutaneous lesions in AIDS-related Kaposi sarcoma.

Limitations of use: Alitretinoin is not indicated when systemic therapy is necessary (eg, >10 new Kaposi sarcoma lesions in previous month, symptomatic visceral involvement, symptomatic pulmonary Kaposi sarcoma, symptomatic lymphedema). There is no experience in using alitretinoin (topical) in combination with systemic treatment for Kaposi sarcoma.

Contraindications

Known hypersensitivity to alitretinoin, other retinoids, or any component of the formulation

Dosing: Adult

Kaposi sarcoma: Topical: Initial: Apply gel twice daily to cutaneous lesions; may gradually increase application frequency to 3 or 4 times daily based on lesion tolerance. Continue as long as deriving clinical benefit; response may be observed within 2 weeks of initiation, but typically a longer period is required (>14 weeks); in clinical trials, therapy lasted up to 96 weeks.

Dosage adjustment for concomitant therapy: Significant drug interactions exist, requiring dose/frequency adjustment or avoidance. Consult drug interactions database for more information.

Dosing: Adjustment for Toxicity

Application site irritation: May reduce the frequency of administration if application site toxicity occurs.

Grades 0, 1, or 2 dermal irritation: No dosage adjustment necessary (Walmsley 1999).

Grade 3 dermal irritation: Reduce dosing frequency to once daily (Bodsworth 2001) or reduce frequency or withhold treatment for up to 2 weeks and restart when irritation improves to grade 1 or lower (Walmsley 1999).

Grade 4 dermal irritation: Discontinue treatment until irritation improves to grade 1 or lower within 2 weeks and then restart at less than once daily for 2 weeks before increasing application frequency. If grade 4 irritation occurs less than once daily, do not restart treatment (Walmsley 1999).

Administration

Topical: Apply sufficient gel to cover lesion(s) with a generous coating; allow gel to dry 3 to 5 minutes after application before covering with clothing. Do not cover alitretinoin application site with occlusive dressings. Avoid applying gel to normal skin surrounding lesions. Do not apply to any lesions on or near mucosal surfaces.

Storage

Store at 25°C (77°F); excursions permitted between 15°C to 30°C (59°F to 86°F).

Drug Interactions

Aminolevulinic Acid (Systemic): Photosensitizing Agents may enhance the photosensitizing effect of Aminolevulinic Acid (Systemic). Avoid combination

Aminolevulinic Acid (Topical): Photosensitizing Agents may enhance the photosensitizing effect of Aminolevulinic Acid (Topical). Monitor therapy

Multivitamins/Fluoride (with ADE): May enhance the adverse/toxic effect of Retinoic Acid Derivatives. Avoid combination

Multivitamins/Minerals (with ADEK, Folate, Iron): May enhance the adverse/toxic effect of Retinoic Acid Derivatives. Avoid combination

Multivitamins/Minerals (with AE, No Iron): May enhance the adverse/toxic effect of Retinoic Acid Derivatives. Avoid combination

Porfimer: Photosensitizing Agents may enhance the photosensitizing effect of Porfimer. Monitor therapy

Tetracyclines: May enhance the adverse/toxic effect of Retinoic Acid Derivatives. The development of pseudotumor cerebri is of particular concern. Avoid combination

Verteporfin: Photosensitizing Agents may enhance the photosensitizing effect of Verteporfin. Monitor therapy

Adverse Reactions

>10%:

Central nervous system: Pain (≤34%), paresthesia (3% to 22%)

Dermatologic: Skin rash (25% to 77%), pruritus (8% to 11%)

1% to 10%:

Cardiovascular: Edema (3% to 8%)

Dermatologic: Exfoliative dermatitis (3% to 9%), dermatological disease (≤8%)

Warnings/Precautions

Concerns related to adverse effects:

• Dermal irritation: Application site irritation and pain have been reported, including grade 3 dermal irritation; may require dosage reduction.

• Photosensitivity: Alitretinoin may be photosensitizing (based on experience with other retinoids); minimize sun or other UV exposure of treated areas.

Other warnings/precautions:

• Products containing DEET: Do not use concurrently with topical products containing DEET (eg, insect repellant); an increase in DEET toxicity has been observed.

Reproductive Considerations

Females of reproductive potential should avoid becoming pregnant during treatment with topical alitretinoin.

Pregnancy Considerations

Alitretinoin may cause fetal harm if significant absorption occurs in a female who is pregnant.

Patient Education

What is this drug used for?

• It is used to treat skin wounds in patients with AIDS-related Kaposi's sarcoma.

WARNING/CAUTION: Even though it may be rare, some people may have very bad and sometimes deadly side effects when taking a drug. Tell your doctor or get medical help right away if you have any of the following signs or symptoms that may be related to a very bad side effect:

• Burning or numbness feeling

• Swelling

• Severe skin irritation

• Signs of an allergic reaction, like rash; hives; itching; red, swollen, blistered, or peeling skin with or without fever; wheezing; tightness in the chest or throat; trouble breathing, swallowing, or talking; unusual hoarseness; or swelling of the mouth, face, lips, tongue, or throat.

Note: This is not a comprehensive list of all side effects. Talk to your doctor if you have questions.

Consumer Information Use and Disclaimer: This information should not be used to decide whether or not to take this medicine or any other medicine. Only the healthcare provider has the knowledge and training to decide which medicines are right for a specific patient. This information does not endorse any medicine as safe, effective, or approved for treating any patient or health condition. This is only a limited summary of general information about the medicine's uses from the patient education leaflet and is not intended to be comprehensive. This limited summary does NOT include all information available about the possible uses, directions, warnings, precautions, interactions, adverse effects, or risks that may apply to this medicine. This information is not intended to provide medical advice, diagnosis or treatment and does not replace information you receive from the healthcare provider. For a more detailed summary of information about the risks and benefits of using this medicine, please speak with your healthcare provider and review the entire patient education leaflet.

Further information

Always consult your healthcare provider to ensure the information displayed on this page applies to your personal circumstances.