Targretin
bexarotene · Capsule, Liquid Filled · Oral, Topical
Uses
1 INDICATIONS AND USAGE 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. TARGRETIN (bexarotene) is a retinoid indicated for the treatment of cutaneous manifestations of cutaneous T-cell lymphoma in patients who are refractory to at least one prior systemic therapy. ( 1 )
Dosage and administration
The recommended initial dose of TARGRETIN is 300 mg/m 2 /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 [ see Use in Specific Populations (8.1) ]. Table 1: TARGRETIN Initial Dose Calculation According to Body Surface Area Initial Dose Level (300 mg/m 2 /day) Number of 75 mg TARGRETIN Capsules Body Surface Area (m 2 ) 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/m 2 /day dose level of TARGRETIN may be adjusted to 200 mg/m 2 /day then to 100 mg/m 2 /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/m 2 /day is well tolerated, the dose may be escalated to 400 mg/m 2 /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.
• Recommended initial dose is 300 mg/m 2 /day. ( 2 )
• Take TARGRETIN as a single oral daily dose with a meal. ( 2 )
• Dose Adjustment: May be adjusted to 200 mg/m 2 /day then to 100 mg/m 2 /day. ( 2 )
Dosage forms and strengths
Capsules: 75 mg, off-white, oblong soft gelatin capsules, imprinted with black ink “Targretin”. Capsules: 75 mg ( 3 )
Contraindications
• Pregnancy (Boxed Warning, 4.1 )
• Known hypersensitivity to bexarotene ( 4.2 ) 4.1 Pregnancy TARGRETIN 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. 4.2 Hypersensitivity TARGRETIN Capsules are contraindicated in patients with a known serious hypersensitivity to bexarotene or other components of the product.
Warnings and precautions
• Hyperlipidemia: TARGRETIN causes elevations in blood lipids. Obtain baseline values, monitor, and manage elevations during therapy by dose reduction, interruption, discontinuation and/or lipid lowering therapy. ( 5.1 , 5.11 )
• Pancreatitis: Interrupt TARGRETIN and evaluate if suspected. ( 5.2 )
• Hepatotoxicity, Cholestasis, and Hepatic Failure: Interrupt or discontinue TARGRETIN and evaluate if liver chemistry tests exceed three times the upper limit of normal values. ( 5.3 )
• Hypothyroidism: TARGRETIN therapy can cause hypothyroidism. Monitor and replace thyroid hormone if needed. ( 5.5 )
• Neutropenia: Monitor for neutropenia. Reduce TARGRETIN dose or interrupt as indicated. ( 5.6 )
• Photosensitivity: Minimize exposure to sunlight and artificial ultraviolet light during treatment. ( 5.10 ) 5.1 Hyperlipidemia TARGRETIN induces substantial elevations in lipids in most patients. About 70% of patients with CTCL who received an initial dose of > 300 mg/m 2 /day of TARGRETIN had fasting triglyceride levels greater than 2.5 times the upper limit of normal. About 55% had values over 800 mg/dL with a median of about 1200 mg/dL in those patients. Cholesterol elevations above 300 mg/dL occurred in approximately 60% and 75% of patients with CTCL who received an initial dose of 300 mg/m 2 /day or greater than 300 mg/m 2 /day, respectively. Decreases in high density lipoprotein (HDL) cholesterol to less than 25 mg/dL were seen in about 55% and 90% of patients receiving an initial dose of 300 mg/m 2 /day or greater than 300 mg/m 2 /day, respectively, of TARGRETIN. Monitor lipid changes and treat abnormalities during therapy. The effects on triglycerides, HDL cholesterol, and total cholesterol were reversible with cessation of therapy, and could generally be mitigated by dose reduction and/or concomitant antilipemic therapy. Perform fasting blood lipid determinations before TARGRETIN therapy is initiated and weekly until the lipid response to TARGRETIN is established, which usually occurs within 2 to 4 weeks, and monitor at 8-week intervals thereafter. Fasting triglycerides should be normal or normalized with appropriate intervention prior to initiating TARGRETIN therapy. Maintain triglyceride levels below 400 mg/dL to reduce the risk of clinical sequelae [ see Warnings and Precautions (5.2) ]. If fasting triglycerides are elevated or become elevated during treatment, institute antilipemic therapy, and if necessary, reduce or interrupt the dose of TARGRETIN. In the 300 mg/m 2 /day initial dose group, 60% of patients were given lipid lowering drugs. Atorvastatin was used in 48% (73/152) of patients with CTCL. Because of a potential drug-drug interaction, avoid gemfibrozil use with TARGRETIN [ see Drug Interactions (7) ]. 5.2 Pancreatitis Acute pancreatitis, including a fatal case, has been reported in four patients with CTCL and in six patients with non-CTCL cancers treated with TARGRETIN; the cases were associated with marked elevations of fasting serum triglycerides, the lowest being 770 mg/dL in one patient. One patient with advanced non-CTCL cancer died of pancreatitis. Interrupt TARGRETIN and evaluate if pancreatitis is suspected. Patients with CTCL who have risk factors for pancreatitis (e.g., prior pancreatitis, uncontrolled hyperlipidemia, excessive alcohol consumption, uncontrolled diabetes mellitus, biliary tract disease, and medications known to increase triglyceride levels or to be associated with pancreatic toxicity) may be at greater risk for pancreatitis associated with TARGRETIN [ see Warnings and Precautions (5.1) ]. 5.3 Hepatotoxicity, Cholestasis, and Hepatic Failure TARGRETIN caused elevations in liver chemistry tests (LFTs) in 5% (AST), 2% (ALT), and 0% (bilirubin) in patients with CTCL receiving an initial dose of 300 mg/m 2 /day. In contrast, with an initial dose greater than 300 mg/m 2 /day of TARGRETIN, the incidence of LFT elevations was higher at 7% (SGOT/AST), 9% (SGPT/ALT), and 6% (bilirubin). Two patients developed cholestasis, including one patient who died of liver failure. In clinical trials, elevated LFTs resolved within 1 month in 80% of patients following a decrease in dose or discontinuation of therapy. Obtain baseline LFTs and monitor LFTs after 1, 2, and 4 weeks of treatment initiation, and if stable, at least every 8 weeks thereafter during treatment. Interrupt or discontinue TARGRETIN if test results exceed three times the upper limit of normal values for AST, ALT, or bilirubin. 5.4 Hypothyroidism TARGRETIN induces hypothyroidism in about half of all patients treated by causing a reversible reduction in levels of thyroid hormone (total thyroxine [total T4]) and thyroid-stimulating hormone (TSH). The incidence of decreases in TSH and total T4 were about 60% and 45%, respectively, in patients with CTCL receiving an initial dose of 300 mg/m 2 /day. Hypothyroidism was reported as an adverse event in 29% of patients. Consider treatment with thyroid hormone supplementation in patients with hypothyroidism. In the 300 mg/m 2 /day initial dose group, 37% of patients were treated with thyroid hormone replacement. Obtain baseline thyroid function tests and patients monitor during treatment. 5.5 Neutropenia Leukopenia in the range of 1000 to <3000 WBC x 10 6 /L occurred in 18% of patients with CTCL receiving an initial dose of 300 mg/m 2 /day of TARGRETIN. Patients receiving an initial dose greater than 300 mg/m 2 /day of TARGRETIN had an incidence of leukopenia of 43%. No patient with CTCL treated with TARGRETIN developed leukopenia of less than 1000 WBC x 10 6 /L. The usual time to onset of leukopenia was 4 to 8 weeks after initiating TARGRETIN. The leukopenia observed in most patients was predominantly neutropenia. In the 300 mg/m 2 /day initial dose group, the incidence of NCI Grade 3 and Grade 4 neutropenia, respectively, was 12% and 4%.
Side effects
The following serious adverse reactions are discussed in greater detail in other sections of the prescribing information:
• Hyperlipidemia [ see Warnings and Precautions (5.1) ]
• Pancreatitis [ see Warnings and Precautions (5.2) ]
• Hepatotoxicity, Cholestasis, and Hepatic Failure [ see Warnings and Precautions (5.3) ]
• Hypothyroidism [ see Warnings and Precautions (5.4) ]
• Neutropenia [ see Warnings and Precautions (5.5) ]
• Cataracts [ see Warnings and Precautions (5.6) ]
• Vitamin A Supplementation Hazard [ see Warnings and Precautions (5.7) ]
• Hypoglycemia Risk in Patients with Diabetes Mellitus [ see Warnings and Precautions (5.8) ]
• Photosensitivity [ see Warnings and Precautions (5.9) ]
• Laboratory Tests [ see Warnings and Precautions (5.10) ]
• Drug/Laboratory Test Interactions [ see Warnings and Precautions (5.11) ] The most common adverse reactions (greater than 10%) include: hyperlipidemia, hypercholesteremia, headache, hypothyroidism, asthenia, leukopenia, rash, nausea, infection, peripheral edema, abdominal pain, and dry skin. ( 6.1 ) To report SUSPECTED ADVERSE REACTIONS, contact Bausch Health US, LLC at 1-800-321-4576 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch. 6.1 Clinical Trials Experience Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in practice. The safety of TARGRETIN has been evaluated in two clinical trials of 152 patients with CTCL who received TARGRETIN for up to 97 weeks and in 352 patients in other trials. The mean duration of therapy for the 152 patients with CTCL was 166 days. The most common adverse events reported with an incidence of at least 10% in patients with CTCL treated at an initial dose of 300 mg/m 2 /day of TARGRETIN are shown in Table 2. The events at least possibly related to treatment are lipid abnormalities (elevated triglycerides, elevated total and LDL cholesterol and decreased HDL cholesterol), hypothyroidism, headache, asthenia, rash, leukopenia, anemia, nausea, infection, peripheral edema, abdominal pain, and dry skin. Most adverse events occurred at a greater incidence in patients treated at starting doses of greater than 300 mg/m 2 /day (see Table 2). Adverse reactions leading to TARGRETIN dose reduction or discontinuation in at least two patients were hyperlipemia, neutropenia/leukopenia, diarrhea, fatigue/lethargy, hypothyroidism, headache, liver function test abnormalities, rash, pancreatitis, nausea, anemia, allergic reaction, muscle spasm, pneumonia, and confusion. The NCI Grade 3 and NCI Grade 4 adverse reactions reported in two or more patients with CTCL treated at an initial dose of 300 mg/m 2 /day of TARGRETIN (see Table 3) were hypertriglyceridemia, pruritus, headache, peripheral edema, leukopenia, rash, and hypercholesteremia. Most of these moderately severe or severe adverse events occurred at a higher rate in patients treated at starting doses of greater than 300 mg/m 2 /day than in patients treated at a starting dose of 300 mg/m 2 /day. In patients with CTCL receiving an initial dose of 300 mg/m 2 /day, the incidence of NCI Grade 3 or 4 elevations in triglycerides and total cholesterol was 28% and 25%, respectively (Table 4). In contrast, in patients with CTCL receiving greater than 300 mg/m 2 /day, the incidence of NCI Grade 3 or 4 elevated triglycerides and total cholesterol was 45% and 45%, respectively. Other Grade 3 and 4 laboratory abnormalities are shown in Table 3. In addition to the 152 patients enrolled in the two CTCL trials, 352 patients received TARGRETIN as monotherapy for various advanced malignancies at doses from 5 mg/m 2 /day to 1000 mg/m 2 /day. The common adverse reactions (incidence greater than 10%) were similar to those seen in patients with CTCL. In the 504 patients (CTCL and non-CTCL) who received TARGRETIN as monotherapy, drug-related serious adverse reactions that were fatal, in one patient each, were acute pancreatitis, subdural hematoma, and liver failure. In the patients with CTCL receiving an initial dose of 300 mg/m 2 /day of TARGRETIN, adverse reactions reported at an incidence of less than 10% and not included in Tables 2 through 4 or discussed in other parts of labeling and possibly related to treatment were as follows: Body as a Whole: chills, cellulitis, chest pain, breast pain, sepsis, and monilia infection. Cardiovascular: hemorrhage, hypertension, angina pectoris, right heart failure, syncope, and tachycardia. Digestive: constipation, dry mouth, flatulence, colitis, dyspepsia, cheilitis, gastroenteritis, gingivitis, liver failure, and melena. Hemic and Lymphatic: eosinophilia, thrombocythemia, coagulation time increased, lymphocytosis, and thrombocytopenia. Metabolic and Nutritional: LDH increased, creatinine increased, hypoproteinemia, hyperglycemia, weight decreased, weight increased, and amylase increased. Musculoskeletal: arthralgia, myalgia, bone pain, myasthenia, and arthrosis. Nervous: depression, agitation, ataxia, cerebrovascular accident, confusion, dizziness, hyperesthesia, hypesthesia, and neuropathy. Respiratory: pharyngitis, rhinitis, dyspnea, pleural effusion, bronchitis, cough increased, lung edema, hemoptysis, and hypoxia. Skin and Appendages: skin ulcer, acne, alopecia, skin nodule, macular papular rash, pustular rash, serous drainage, and vesicular bullous rash. Special Senses: dry eyes, conjunctivitis, ear pain, blepharitis, corneal lesion, keratitis, otitis externa, and visual field defect. Urogenital: albuminuria, hematuria, urinary incontinence, urinary tract infection, urinary urgency, dysuria, and kidney function abnormal.
Drug interactions
Effect of Other Drugs on TARGRETIN Gemfibrozil: Concomitant administration of TARGRETIN and gemfibrozil resulted in increases in plasma concentrations of bexarotene. Concomitant administration of gemfibrozil with TARGRETIN is not recommended. Effect of TARGRETIN on Other Drugs TARGRETIN may be an inducer for the CYP3A4 enzymes, and may reduce plasma concentrations of other substrates metabolized by CYP3A4. Drug products which may be affected include oral or other systemic hormonal contraceptives. Thus, if treatment with TARGRETIN is intended for a female with reproductive potential, it is strongly recommended that a non-hormonal contraception be considered. [ see Use in Specific Populations (8.3) , Clinical Pharmacology (12.3) ]. Laboratory Test Interference CA125 assay values in patients with ovarian cancer may be increased by TARGRETIN therapy.
Use in specific populations
8.1 Pregnancy Risk Summary 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 [see Data] . TARGRETIN must not be given to a pregnant female or a female who intends to become pregnant. If pregnancy does occur during treatment with TARGRETIN, immediately discontinue the drug and advise the pregnant female of the potential risk to a fetus. 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. Data Animal Data 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). 8.2 Lactation Risk Summary There is no information regarding the presence of TARGRETIN in human milk, the effects on the breast fed infant, or the effects on milk production. Because many drugs are excreted in human milk and because of the potential for serious adverse reactions in nursing infants from TARGRETIN, discontinue breastfeeding during treatment with TARGRETIN. 8.3 Females and Males of Reproductive Potential Pregnancy Testing Obtain a negative serum pregnancy test (e.g., serum beta-human chorionic gonadotropin [beta-HCG]) with a sensitivity of at least 50 mIU/L within 1 week prior to TARGRETIN therapy. Obtain another pregnancy test at monthly intervals while the patient remains on TARGRETIN. Contraception Females TARGRETIN can cause fetal harm when administered to a pregnant female [ see Use in Specific Populations (8.1) ]. Females of reproductive potential should be advised to avoid becoming pregnant when TARGRETIN is used. Effective contraception must be used for 1 month prior to the initiation of therapy, during therapy and for at least 1 month following discontinuation of therapy; it is recommended that two reliable forms of contraception be used simultaneously unless abstinence is the chosen method. Bexarotene can potentially induce metabolic enzymes and thereby theoretically reduce the plasma concentrations of oral or other systemic hormonal contraceptives [ see Drug Interactions (7) ]. Thus, if treatment with TARGRETIN is intended in a female with reproductive potential, it is strongly recommended that one of the two reliable forms of contraception should be non-hormonal. TARGRETIN therapy should be initiated on the second or third day of a normal menstrual period. No more than a 1-month supply of TARGRETIN should be given to the patient so that the results of pregnancy testing can be assessed and counseling regarding avoidance of pregnancy and birth defects can be reinforced. Males Male patients with sexual partners who are pregnant, possibly pregnant, or who could become pregnant must use condoms during sexual intercourse while taking TARGRETIN and for at least 1 month after the last dose of drug. 8.4 Pediatric Use Safety and effectiveness of TARGRETIN in pediatric patients have not been established. 8.5 Geriatric Use Of the total patients with CTCL in clinical trials of TARGRETIN, 64% were 60 years or older, while 33% were 70 years or older. No overall differences in safety were observed between patients 70 years or older and younger patients, but greater sensitivity of some older individuals to TARGRETIN cannot be ruled out. Responses to TARGRETIN were observed across all age group decades, without preference for any individual age group decade. 8.6 Hepatic Impairment No specific studies have been conducted with TARGRETIN in subjects with hepatic impairment. Hepatic impairment is expected to lead to decreased clearance [ see Clinical Pharmacology (12.3) ]. If TARGRETIN is used in patients with hepatic impairment, monitor for signs of toxicity that may be due to increased exposure.
Pregnancy
8.1 Pregnancy Risk Summary 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 [see Data] . TARGRETIN must not be given to a pregnant female or a female who intends to become pregnant. If pregnancy does occur during treatment with TARGRETIN, immediately discontinue the drug and advise the pregnant female of the potential risk to a fetus. 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. Data Animal Data 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).
Pediatric use
8.4 Pediatric Use Safety and effectiveness of TARGRETIN in pediatric patients have not been established.
Geriatric use
8.5 Geriatric Use Of the total patients with CTCL in clinical trials of TARGRETIN, 64% were 60 years or older, while 33% were 70 years or older. No overall differences in safety were observed between patients 70 years or older and younger patients, but greater sensitivity of some older individuals to TARGRETIN cannot be ruled out. Responses to TARGRETIN were observed across all age group decades, without preference for any individual age group decade.
Overdosage
Doses up to 1000 mg/m 2 /day of TARGRETIN have been administered in short-term trials in patients with advanced cancer without acute toxic effects. Single doses of 1500 mg/kg and 720 mg/kg were tolerated without significant toxicity in rats and dogs, respectively. These doses are approximately 30 and 50 times, respectively, the recommended human dose on a mg/m 2 basis.
Description
11 DESCRIPTION TARGRETIN ® (bexarotene) Capsules contain bexarotene, a member of a subclass of retinoids that selectively activate retinoid X receptors (RXRs). These retinoid receptors have biologic activity distinct from that of retinoic acid receptors (RARs). The chemical name of bexarotene is 4-[1-(5,6,7,8-tetrahydro-3,5,5,8,8-pentamethyl-2-naphthalenyl)ethenyl]benzoic acid, and the structural formula is as follows: Bexarotene is an off-white to white powder with a molecular weight of 348.48 and a molecular formula of C 24 H 28 O 2 . It is insoluble in water and slightly soluble in vegetable oils and ethanol, USP. Each TARGRETIN capsule contains 75 mg of bexarotene for oral administration. It also contains the following inactive ingredients: butylated hydroxyanisole, NF, polyethylene glycol 400, NF, polysorbate 20, NF, and povidone, USP. The capsule shell contains gelatin, NF, sorbitol special glycerin blend, and titanium dioxide, USP. Description
Mechanism of action
12.1 Mechanism of Action Bexarotene selectively binds and activates retinoid X receptor subtypes (RXRα, RXRß, RXRγ). RXRs can form heterodimers with various receptor partners such as retinoic acid receptors (RARs), vitamin D receptor, thyroid receptor, and peroxisome proliferator activator receptors (PPARs). Once activated, these receptors function as transcription factors that regulate the expression of genes that control cellular differentiation and proliferation. Bexarotene inhibits the growth in vitro of some tumor cell lines of hematopoietic and squamous cell origin. It also induces tumor regression in vivo in some animal models. The exact mechanism of action of bexarotene in the treatment of cutaneous T-cell lymphoma (CTCL) is unknown.
How supplied
16 HOW SUPPLIED/STORAGE AND HANDLING TARGRETIN ® (bexarotene) Capsules are supplied as 75 mg off-white, oblong soft gelatin capsules, imprinted with “Targretin”, in high density polyethylene bottles with child-resistant closures. Bottles of 100 capsules: NDC 0187-5526-75 Store at 2° to 25°C (36° to 77°F). Avoid exposing to high temperatures and humidity after the bottle is opened. Protect from light.
Patient information
Advise the patient to read the FDA-approved patient labeling (Patient Information). Inform the patient or caregiver about the following: Birth Defects Advise patients that TARGRETIN is contraindicated in pregnancy [see Contraindications (4.1) ]. TARGRETIN is a member of the retinoid class of drugs that is associated with birth defects in humans [see Use In Specific Populations (8.1) ].
• Advise females of reproductive potential that they must avoid pregnancy while taking TARGRETIN and for at least 1 month following discontinuation of therapy.
• Advise females of reproductive potential of the importance of monthly pregnancy testing while taking TARGRETIN.
• Advise females of reproductive potential to use effective contraception for 1 month prior to the initiation of therapy, during therapy, and for at least 1 month following discontinuation of therapy and that two reliable forms of contraception should be used simultaneously, one of which should be non-hormonal.
• Advise females of reproductive potential that TARGRETIN therapy should be initiated on the second or third day of a normal menstrual period.
• Instruct patient to immediately stop taking TARGRETIN if she becomes pregnant while taking this drug.
• Advise male patients with sexual partners who are pregnant, possibly pregnant, or who could become pregnant that they must use condoms during sexual intercourse while taking TARGRETIN and for at least 1 month after the last dose of the drug. Pancreatitis Advise patients of the risk of developing pancreatitis, which may be accompanied by nausea, vomiting, and abdominal or back pain and to immediately contact their healthcare provider if these symptoms occur [see Warnings and Precautions (5.2) ]. Hepatotoxicity Inform patients of the possibility of developing liver function abnormalities and serious hepatic toxicity. Advise patients to immediately contact their healthcare provider if signs of liver failure occur, including jaundice, anorexia, bleeding, or bruising [see Warnings and Precautions (5.3) ]. Neutropenia Advise patients of the possibility of developing neutropenia and to immediately contact their healthcare provider should they develop a fever, particularly in association with any suggestion of infection [see Warnings and Precautions (5.5) ]. Cataracts Advise patients of the possibility of developing new or worsening cataracts and to inform their healthcare provider about any changes in their vision during treatment with TARGRETIN [see Warnings and Precautions (5.6) ]. Vitamin A Supplementation Hazard Advise patients to limit vitamin A intake to ≤15,000 IU/day to avoid potential additive toxic effects. Hypoglycemia and Diabetes Mellitus Advise patients of the possibility of developing hypoglycemia when using insulin, agents enhancing insulin secretion, or insulin sensitizers while on TARGRETIN therapy. Instruct patients on these medications to check their blood sugar frequently and to notify their physicians of any changes in blood sugar level [see Warnings and Precautions (5.8) ]. Photosensitivity Advise patients of potential increased skin sensitivity to sunlight while taking TARGRETIN and to minimize exposure to sunlight and artificial ultraviolet light [see Warnings and Precautions (5.9) ]. Laboratory Tests Advise patients of laboratory testing which will occur during therapy to monitor lipids, liver function, thyroid function, and white blood cell counts [see Warnings and Precautions (5.10) ]. If applicable, advise patients of monthly pregnancy testing [see Use In Specific Populations (8.3) ]. Administration Instructions Advise patients to take TARGRETIN with a meal [see DOSAGE AND ADMINISTRATION ]. Distributed by: Bausch Health US, LLC Bridgewater, NJ 08807 USA Manufactured by: Catalent Pharma Solutions LLC St. Petersburg, FL 33716 USA TARGRETIN is a trademark of Bausch Health Companies Inc. or its affiliates. Any other product/brand names are trademarks of their respective owners. © 2020 Bausch Health Companies Inc. or its affiliates 9436601
Label text from the FDA structured product label by Bausch Health US, LLC (revised Apr 30, 2020). Long sections are shortened; the complete label is on DailyMed.
Active ingredients
- Bexarotene in 2 products
Targretin NDC products (2)
| NDC | Strength & form | Labeler | Type |
|---|---|---|---|
| 0187-5525 | Bexarotene 1 g/100g Gel | Bausch Health US, LLC | NDA |
| 0187-5526 | Bexarotene 75 mg/1 Capsule, Liquid Filled | Bausch Health US, LLC | NDA |
Frequently asked questions
What is Targretin used for?
1 INDICATIONS AND USAGE 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. TARGRETIN (bexarotene) is a retinoid indicated for the treatment of cutaneous manifestations of cutaneous T-cell lymphoma in patients who are refractory to at least one prior…
What are the side effects of Targretin?
The following serious adverse reactions are discussed in greater detail in other sections of the prescribing information: • Hyperlipidemia [ see Warnings and Precautions (5.1) ] • Pancreatitis [ see Warnings and Precautions (5.2) ] • Hepatotoxicity, Cholestasis, and Hepatic Failure [ see Warnings and Precautions (5.3) ] • Hypothyroidism [ see Warnings and Precautions (5.4) ] • Neutropenia [ see… See the full label for the complete list.
Who makes Targretin?
Targretin is listed by 1 labeler in the FDA NDC directory, including Bausch Health US, LLC.