TEGISON

Clinical safety rating: caution

Comprehensive clinical and safety monograph for TEGISON (TEGISON).

How it works

Retinoid that binds to nuclear retinoic acid receptors (RARs) and retinoid X receptors (RXRs), modulating gene transcription involved in cell differentiation, proliferation, and apoptosis. It reduces epidermal proliferation and promotes normal keratinization.

What the body does with it

Metabolism	Metabolized in the liver via isomerization and glucuronidation; undergoes enterohepatic circulation. Active metabolite: all-trans-retinoic acid and other isomers. Main enzyme: CYP2C8, CYP3A4.
Excretion	Primarily renal (60-80% as metabolites) and biliary/fecal (15-25% as unchanged drug and metabolites).
Half-life	Terminal elimination half-life is approximately 120-168 hours (5-7 days) due to extensive tissue storage; clinical effects persist for weeks after discontinuation.
Protein binding	≥ 99.9% bound to albumin and lipoproteins.
Volume of Distribution	Approximately 1.5-2.0 L/kg, indicating extensive tissue distribution, particularly in adipose tissue and liver.
Bioavailability	Oral bioavailability is highly variable, approximately 60-70% when taken with food; absorption is enhanced by a high-fat meal.
Onset of Action	Peak plasma concentrations reached 3-5 hours after oral administration; clinical improvement in psoriasis typically noted after 2-4 weeks.
Duration of Action	Therapeutic effects can persist for 2-3 months after cessation due to slow elimination; adverse effects may resolve more slowly.

Classification & Brands

Dosing & administration

Initial dose: 0.5-1 mg/kg/day orally, divided twice daily; maintenance dose: 0.3-0.5 mg/kg/day. Maximum dose: 1.5 mg/kg/day.

Dosage form	CAPSULE
Renal impairment	eGFR >60 mL/min: no adjustment. eGFR 30-60: reduce dose by 25%. eGFR <30: use with caution, consider 50% dose reduction.
Liver impairment	Child-Pugh A: no adjustment. Child-Pugh B: reduce dose by 50%. Child-Pugh C: contraindicated.
Pediatric use	0.5-1 mg/kg/day orally, divided twice daily; not recommended for children <2 years due to risk of premature epiphyseal closure.
Geriatric use	Start at lower end of dosing range (0.5 mg/kg/day); monitor for renal function and adjust accordingly.

Use during pregnancy

1st trimester	Consult provider
2nd trimester	Consult provider
3rd trimester	Consult provider

Clinical note

Comprehensive clinical and safety monograph for TEGISON (TEGISON).

Breastfeeding	Etretinate is excreted in human milk; M/P ratio not established. Due to potential for serious adverse reactions in nursing infants, breastfeeding is contraindicated during therapy and for at least 3 years after last dose.
Teratogenic Risk	Tegison (etretinate) is a teratogen. Contraindicated in pregnancy. Fetal risk: major congenital malformations (CNS, cardiovascular, craniofacial) with any exposure. First trimester: highest risk; second/third trimester: also risk but less data. Pregnancy Category X. Must avoid pregnancy for at least 3 years after discontinuation due to prolonged elimination.

Warnings & precautions

■ FDA Black Box Warning

Contraindicated in women of childbearing potential unless they use effective contraception during and 3 years after therapy due to extremely high risk of severe birth defects (teratogenicity).

Side Effect Profile

Serious Effects

Absolute Contraindications

Pregnancy or women of childbearing potential not using effective contraception, lactation, hypersensitivity to retinoids, severe hepatic impairment, hypervitaminosis A, concurrent use of tetracyclines (increased risk of pseudotumor cerebri).

Clinical Precautions

Precautions

Teratogenicity (must avoid pregnancy), hepatotoxicity (monitor LFTs), hyperlipidemia (monitor lipids), pseudotumor cerebri (risk with tetracyclines), skeletal hyperostosis, pancreatitis, mood changes/depression, photosensitivity, corneal opacities, decreased night vision.

Clinical Tips & Counseling

Drug interactions

Loading safety data…

TEGISON

Clinical safety rating: caution

Comprehensive clinical and safety monograph for TEGISON (TEGISON).

How it works

What the body does with it

Metabolism	Metabolized in the liver via isomerization and glucuronidation; undergoes enterohepatic circulation. Active metabolite: all-trans-retinoic acid and other isomers. Main enzyme: CYP2C8, CYP3A4.
Excretion	Primarily renal (60-80% as metabolites) and biliary/fecal (15-25% as unchanged drug and metabolites).
Half-life	Terminal elimination half-life is approximately 120-168 hours (5-7 days) due to extensive tissue storage; clinical effects persist for weeks after discontinuation.
Protein binding	≥ 99.9% bound to albumin and lipoproteins.
Volume of Distribution	Approximately 1.5-2.0 L/kg, indicating extensive tissue distribution, particularly in adipose tissue and liver.
Bioavailability	Oral bioavailability is highly variable, approximately 60-70% when taken with food; absorption is enhanced by a high-fat meal.
Onset of Action	Peak plasma concentrations reached 3-5 hours after oral administration; clinical improvement in psoriasis typically noted after 2-4 weeks.
Duration of Action	Therapeutic effects can persist for 2-3 months after cessation due to slow elimination; adverse effects may resolve more slowly.

Classification & Brands

Dosing & administration

Initial dose: 0.5-1 mg/kg/day orally, divided twice daily; maintenance dose: 0.3-0.5 mg/kg/day. Maximum dose: 1.5 mg/kg/day.

Dosage form	CAPSULE
Renal impairment	eGFR >60 mL/min: no adjustment. eGFR 30-60: reduce dose by 25%. eGFR <30: use with caution, consider 50% dose reduction.
Liver impairment	Child-Pugh A: no adjustment. Child-Pugh B: reduce dose by 50%. Child-Pugh C: contraindicated.
Pediatric use	0.5-1 mg/kg/day orally, divided twice daily; not recommended for children <2 years due to risk of premature epiphyseal closure.
Geriatric use	Start at lower end of dosing range (0.5 mg/kg/day); monitor for renal function and adjust accordingly.

Use during pregnancy

1st trimester	Consult provider
2nd trimester	Consult provider
3rd trimester	Consult provider

Clinical note

Comprehensive clinical and safety monograph for TEGISON (TEGISON).

Breastfeeding	Etretinate is excreted in human milk; M/P ratio not established. Due to potential for serious adverse reactions in nursing infants, breastfeeding is contraindicated during therapy and for at least 3 years after last dose.
Teratogenic Risk	Tegison (etretinate) is a teratogen. Contraindicated in pregnancy. Fetal risk: major congenital malformations (CNS, cardiovascular, craniofacial) with any exposure. First trimester: highest risk; second/third trimester: also risk but less data. Pregnancy Category X. Must avoid pregnancy for at least 3 years after discontinuation due to prolonged elimination.

Warnings & precautions

■ FDA Black Box Warning

Contraindicated in women of childbearing potential unless they use effective contraception during and 3 years after therapy due to extremely high risk of severe birth defects (teratogenicity).