Dosage & Administration
The recommended initial dose of TARGRETIN is 300 mg/m2/day (see Table 1). TARGRETIN should be taken as a single oral daily dose with a meal. For precautions to prevent pregnancy and birth defects in women of child-bearing potential [
TARGRETIN, a retinoid, can cause fetal harm based on findings from animal studies when administered to a pregnant female and is contraindicated during pregnancy. Bexarotene was teratogenic and caused developmental mortality in rats following oral administration during organogenesis
The background risk of major birth defects and miscarriage for the indicated populations is unknown. However, the background risk in the U.S. general population of major birth defects is 2-4% and of miscarriage is 15-20% of clinically recognized pregnancies.
Bexarotene caused malformations when administered orally to pregnant rats during days 7-17 of gestation. Developmental abnormalities included incomplete ossification at 4 mg/kg/day and cleft palate, depressed eye bulge/microphthalmia, and small ears at 16 mg/kg/day. The plasma AUC of bexarotene in rats at 4 mg/kg/day is approximately one third the AUC in humans at the recommended daily dose. At doses greater than 10 mg/kg/day, bexarotene caused developmental mortality. The no effect dose for fetal effects in rats was 1 mg/kg/day (producing an AUC approximately one sixth of the AUC at the recommended human daily dose).
Initial Dose Level (300 mg/m2/day) | Number of 75 mg TARGRETIN Capsules | |
Body Surface Area (m2) | Total Daily Dose (mg/day) | |
0.88 – 1.12 | 300 | 4 |
1.13 – 1.37 | 375 | 5 |
1.38 – 1.62 | 450 | 6 |
1.63 – 1.87 | 525 | 7 |
1.88 – 2.12 | 600 | 8 |
2.13 – 2.37 | 675 | 9 |
2.38 – 2.62 | 750 | 10 |
Dose Modification Guidelines: The 300 mg/m2/day dose level of TARGRETIN may be adjusted to 200 mg/m2/day then to 100 mg/m2/day, or temporarily suspended, if necessitated by toxicity. When toxicity is controlled, doses may be carefully readjusted upward. If there is no tumor response after 8 weeks of treatment and if the initial dose of 300 mg/m2/day is well tolerated, the dose may be escalated to 400 mg/m2/day with careful monitoring.
Duration of Therapy: In clinical trials in CTCL, TARGRETIN was administered for up to 97 weeks.
TARGRETIN should be continued as long as the patient is deriving benefit.
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Targretin Capsules Prescribing Information
TARGRETIN, a retinoid, can cause fetal harm based on findings from animal studies when administered to a pregnant female and is contraindicated during pregnancy. Bexarotene was teratogenic and caused developmental mortality in rats following oral administration during organogenesis
The background risk of major birth defects and miscarriage for the indicated populations is unknown. However, the background risk in the U.S. general population of major birth defects is 2-4% and of miscarriage is 15-20% of clinically recognized pregnancies.
Bexarotene caused malformations when administered orally to pregnant rats during days 7-17 of gestation. Developmental abnormalities included incomplete ossification at 4 mg/kg/day and cleft palate, depressed eye bulge/microphthalmia, and small ears at 16 mg/kg/day. The plasma AUC of bexarotene in rats at 4 mg/kg/day is approximately one third the AUC in humans at the recommended daily dose. At doses greater than 10 mg/kg/day, bexarotene caused developmental mortality. The no effect dose for fetal effects in rats was 1 mg/kg/day (producing an AUC approximately one sixth of the AUC at the recommended human daily dose).
TARGRETIN® (bexarotene) Capsules are indicated for the treatment of cutaneous manifestations of cutaneous T-cell lymphoma in patients who are refractory to at least one prior systemic therapy.
The recommended initial dose of TARGRETIN is 300 mg/m2/day (see Table 1). TARGRETIN should be taken as a single oral daily dose with a meal. For precautions to prevent pregnancy and birth defects in women of child-bearing potential [
TARGRETIN, a retinoid, can cause fetal harm based on findings from animal studies when administered to a pregnant female and is contraindicated during pregnancy. Bexarotene was teratogenic and caused developmental mortality in rats following oral administration during organogenesis
The background risk of major birth defects and miscarriage for the indicated populations is unknown. However, the background risk in the U.S. general population of major birth defects is 2-4% and of miscarriage is 15-20% of clinically recognized pregnancies.
Bexarotene caused malformations when administered orally to pregnant rats during days 7-17 of gestation. Developmental abnormalities included incomplete ossification at 4 mg/kg/day and cleft palate, depressed eye bulge/microphthalmia, and small ears at 16 mg/kg/day. The plasma AUC of bexarotene in rats at 4 mg/kg/day is approximately one third the AUC in humans at the recommended daily dose. At doses greater than 10 mg/kg/day, bexarotene caused developmental mortality. The no effect dose for fetal effects in rats was 1 mg/kg/day (producing an AUC approximately one sixth of the AUC at the recommended human daily dose).
Initial Dose Level (300 mg/m2/day) | Number of 75 mg TARGRETIN Capsules | |
Body Surface Area (m2) | Total Daily Dose (mg/day) | |
0.88 – 1.12 | 300 | 4 |
1.13 – 1.37 | 375 | 5 |
1.38 – 1.62 | 450 | 6 |
1.63 – 1.87 | 525 | 7 |
1.88 – 2.12 | 600 | 8 |
2.13 – 2.37 | 675 | 9 |
2.38 – 2.62 | 750 | 10 |
Dose Modification Guidelines: The 300 mg/m2/day dose level of TARGRETIN may be adjusted to 200 mg/m2/day then to 100 mg/m2/day, or temporarily suspended, if necessitated by toxicity. When toxicity is controlled, doses may be carefully readjusted upward. If there is no tumor response after 8 weeks of treatment and if the initial dose of 300 mg/m2/day is well tolerated, the dose may be escalated to 400 mg/m2/day with careful monitoring.
Duration of Therapy: In clinical trials in CTCL, TARGRETIN was administered for up to 97 weeks.
TARGRETIN should be continued as long as the patient is deriving benefit.
Capsules: 75 mg, off-white, oblong soft gelatin capsules, imprinted with black ink “Targretin”.
TARGRETIN, a retinoid, can cause fetal harm based on findings from animal studies when administered to a pregnant female and is contraindicated during pregnancy. Bexarotene was teratogenic and caused developmental mortality in rats following oral administration during organogenesis
The background risk of major birth defects and miscarriage for the indicated populations is unknown. However, the background risk in the U.S. general population of major birth defects is 2-4% and of miscarriage is 15-20% of clinically recognized pregnancies.
Bexarotene caused malformations when administered orally to pregnant rats during days 7-17 of gestation. Developmental abnormalities included incomplete ossification at 4 mg/kg/day and cleft palate, depressed eye bulge/microphthalmia, and small ears at 16 mg/kg/day. The plasma AUC of bexarotene in rats at 4 mg/kg/day is approximately one third the AUC in humans at the recommended daily dose. At doses greater than 10 mg/kg/day, bexarotene caused developmental mortality. The no effect dose for fetal effects in rats was 1 mg/kg/day (producing an AUC approximately one sixth of the AUC at the recommended human daily dose).
• Pregnancy (Boxed Warning,)4.1 PregnancyTARGRETIN can cause fetal harm when administered to a pregnant female. TARGRETIN is a member of the retinoid class of drugs that is associated with birth defects in humans and is contraindicated in females who are pregnant. Bexarotene was also teratogenic and caused developmental mortality when administered orally to pregnant rats. If this drug is used during pregnancy or if the patient becomes pregnant while taking this drug, the patient should be advised of the potential risk to a fetus.
• Known hypersensitivity to bexarotene ()4.2 HypersensitivityTARGRETIN Capsules are contraindicated in patients with a known serious hypersensitivity to bexarotene or other components of the product.