Systemic Therapy Program
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Document Type

Drug Monographs
Treatment Regimens
Scientific Name:
ALITRETINOIN
Brand Name(s):
Panretin®

Drug Monograph

Pharmacology

Mechanism of Action

Alitretinoin (or, 9-cis-retinoic acid) binds to all known intracellular retinoid receptors (RARa, RARb, RARg, RXRa, RXRb, RXRg) which regulate expression of genes that control cellular proliferation and differentiation.  Alitretinoin is a naturally-occuring retinoid in humans.

Pharmacokinetics

Topical Absorption:
minimal absorption (indirect evidence)
Distribution:
No information
Metabolism:
hepatic metabolism to 4-oxo-cis-retinoic acid (major metabolite), and 4-hydroxy-cis-retinoic acid
Metabolized by CYP 2C9, 3A4, 1A1 & 1A2 enzymes
Excretion:
No information

Side Effects

EARLY ONSET (days to weeks)
• Dermal toxicity- rash (25-77%), topical pain (34%), pruritis (8-11%), exfoliative dermatitis (3-9%), paresthesia (3-22%), edema (3-8%).

Therapeutics

Approved Indications

OTHER ONCOLOGY USES (Not Approved in Canada)
• Topical lesions with AIDS-related Kaposi’s sarcoma

Routes

Topical gel

Dosing

Topical:
• Apply to cutaneous Kaposi’s Sarcoma lesions- cover entire lesion and allow gel to dry for 3-5 minutes before covering with clothing.  Avoid application to surrounding normal skin; do not cover lesions near mucous membranes
• Begin with twice daily applications then increase to 3 or 4 times daily as tolerated.
• Do not use occlusive dressings with the gel.

Duration of therapy:
• Treatment should be continued for at least 2 weeks- longer treatment may be required to obtain a local benefit; In clinical trials applications continued for up to 96 weeks

Contraindications

• PREGNANCY (data from animal studies only) • Possible photosensitizer • Hypersensitivity to retinoic acid, Vitamin A, other retinoids or parabens • Caution in patients with cutaneous T-cell lymphoma

Monitoring

Clinical Monitoring

RECOMMENDED CRITERIA
• Daily examination of lesions and surrounding skin for evidence of topical reactions, rash.

Significant Interactions

DEET-containing insect repellants, systemic antiretroviral agents (protease inhibitors, macrolide antibiotics, azole antifungals)- serum concentration may be affected by alitretinoin.

Product Information

Commercial Product Description

Clear yellow gel containing 0.1% Alitretinoin. Not Available in Canada- May be available on a case-by-case basis through Special Access Program.

Pharmaceutical Considerations

Topical Gel:
60 g tubes containing 0.1% alitretinoin.  Also contains dehydrated alcohol, polyehylene glycol 400, hydroxypropyl cellulose and butylated hydroxytoluene. Store at room temperature (25oC).

Handling Risk Level

Pregnancy DKNOWN HAZARDOUS DRUG
FDA Pregnancy Risk Factor D

  • This drug must be handled using precuations outlined in CCNS Policies for Occupational Safety and Administering Cancer Chemotherapy

Note

HANDLING RISK LEVEL:

HAZARD RISK LEVEL 2
FDA Pregnancy Risk Factor D
• This drug must be handled using precuations outlined in CCNS Policies for and Administering Cancer Chemotherapy
• Go to "Additional Information" tab (above) for links to CCNS Policies

NOTE:

Emerging Information
This drug is under investigation and has not been widely used in oncology practice.  As new information is discovered, portions of this monograph may become outdated.  Refer to primary literature and revisions to official product monograph to ensure that information on this drug is current.

Availability & Funding

Administrative Information (Nova Scotia)

• CCNS Provincial Formulary Status- Specialized Level Capital Health Only- Not on Canadian market • Take Home Prescription- Restricted Use • CDHA Formulary Status: Non-Formulary • Pharmacare Formulary Status: Non-Formulary