Table 1.

FDA-approved and acceptable off-label applications of retinoids to treat and prevent skin cancer formation. Proposed mechanisms of action and adverse events included. Abbreviations: AK, Actinic Keratoses; AIDS, Acquired Immunodeficiency Syndrome; CTCL, Cutaneous T-Cell Lympoma; KS, Karposi Sarcoma; MF, Mycosis Fungoides; SOTR, Solid Organ Transplant Recipients.

Name (s)	Trade Names (Manufacturer)	Generation	FDA-Approved Uses for Skin Cancer Management	Off-Label Uses for Skin Cancer Management	Proposed Mechanisms of Action	Adverse Events/Warnings	References
Acitretin	Soriatane (Roche)	Second	None	Oral dosing for KC and AK chemoprevention in SOTR and other at-risk individuals.	High affinity for CRABPII displaces RA and potentiates endogenous RA signaling.	Teratogenicity skeletal abnormalities Hypertriglyceridemia Hyperlipidemia Hepatotoxicity Xerosis	[10,76,209,211]
Adapalene	Differin (Galderma)	Third	None	0.1–0.3% topical formulation for AK treatment	Selective RARγ agonist DNA damage and S-phase arrest in immortalized keratinocytes	Irritation, erythema, burning	[11,113,237]
Alitretinoin 9-cis retinoic acid	Toctino (Basilea)	First	0.1% topical formulation for AIDS-related KS	0.1% topical formulation for non-AIDS related KS. 0.1% topical formulation for CTCL second-line therapy. Oral dosing of 10–30 mg daily used off label for the treatment of CTCL.	RAR-RXR activation Induction of apoptosis in KS cells. Angiogenesis inhibition Inhibition of KSHV replication. G0/G1 cell cycle arrest, apoptosis and modulation of the JAK/STAT pathway.	Teratogenicity Irritation Dermatitis Scaling	[11,202,204,273,275]
Bexarotene Targretin®	Targretin (Ligand)	First	Oral dosing and topical 0.1–1.0% for advance-stage or treatment refractory MF resistant to at least one therapy.	None	Pan-RXR agonist Induction of apoptosis via p53/p73 activation Possible control over skin infiltration colonization by T cells	Teratogenicity irritation, erythema, burning dermatitis	[10,11,197,198,253]
Isotretinoin 13-cis retinoic acid Accutane®	Accutane (Roche), Claravis (Barr), Sotret (Ranbaxy), Amnesteem (Bertek), Absorica (Ranbaxy), Myorisan (VersaPharm)	First	None	Oral dosing for BCC/cSCC chemoprevention in NBCCS and XP.	RAR-RXR activation	Teratogenicity Skeletal abnormalities Hepatotoxicity	[10,11,225,226,278]
Tazarotene Tazorac®	Tazorac (Almirall)	Third	None	0.1% topical formulation for MF treatment as second line therapy	Selective RARγ agonist	Teratogenicity Irritation, erythema, burning	[11,268,269]
Tretinoin, All-trans retinoic acid (ATRA)	Vesanoid (Roche)	First	None	0.1% topical tretinoin to treat AKs.	RAR-RXR activation Induction of keratinocyte apoptosis. Control of hyperproliferative STAT signaling UV protection	Teratogenicity Irritation, erythema	[11,130,131,177,181,279]