Bexarotene 75 mg Capsule, Liquid Filled, 100-count
🆔 Identity & classification
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🏷️ RxNorm drug class
This medicine belongs to the Retinoid class.
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🏭 Manufacturer & labeler
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🩺 Clinical
Bexarotene is used to treat cutaneous T-cell lymphoma (CTCL, a type of lymphoma [cancer] that attacks the skin) in people whose disease could not be treated successfully with at least one other medication. Bexarotene is in a class of medications called retinoids. It works by stopping the growth of cancer cells.
Read the full MedlinePlus article ↗- Bexarotene is used to treat the skin symptoms of a cancer called cutaneous T-cell lymphoma, or CTCL. It's not a traditional chemotherapy — it's a retinoid, meaning it's related to...
- What exactly is bexarotene used for — is it a chemotherapy?
- Bexarotene can affect several important things in your body — your blood fat levels (triglycerides and cholesterol), your liver, your thyroid, and your white blood cell count. Thes...
- Why do I need so many blood tests while I'm on this medication?
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🧪 Inactive Ingredients / Excipients
Inactive ingredients, also called excipients, are components of the drug product other than the active ingredient. They may include fillers, dyes, coatings, preservatives, flavors, or other formulation ingredients.
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IACT rows and label-wide narrative are kept separate; availability and product-level specificity depend on the submitted label.Inactive ingredient FAQ
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💲 Pricing
A drug doesn't have one price. Each row is a different public payment system, and none is what you'd pay at the counter — that depends on your insurance. The ⓘ on each row explains what it measures.
| Price system | Per mL | Per package |
|---|---|---|
| Retail pharmacies payNADAC · weekly | Not in the retail survey — common for institutional, discontinued, or low-volume packs. | |
| Medicaid paysCMS SDUD · 12 mo | No recent Medicaid claims on file for this NDC — rare and low-volume NDCs are suppressed in the public data. | |
| Medicare drug plans payPart D · Q2 2026 | $23.47 | — |
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🔁 Therapeutic equivalents
| Product | Labeler | Pack | NADAC/unit | TE | Status | Price vs. this |
|---|---|---|---|---|---|---|
| Targretin 75 mg 00187-5526-75 | Bausch | 100 capsules | — | AB | FDA listed | — |
| Bexarotene 75 mg 00378-6955-01 | Mylan | 100 capsules | — | AB | FDA listed | — |
| bexarotene 75 mg 00591-2832-01 | Actavis | 100 capsules | — | AB | FDA listed | — |
| Bexarotene 75 mg 00832-0285-00 | Upsher-Smith | 100 capsules | — | AB | FDA listed | — |
| Bexarotene 75 mg 31722-0380-01 | Camber | 100 capsules | — | AB | FDA listed | — |
| Bexarotene 75 mg 42291-0072-01 | AvKARE | 100 capsules | — | AB | FDA listed | — |
| Bexarotene 75 mgthis 43975-0315-10 | ANI | 100 capsules | — | AB | FDA listed | — |
| Bexarotene 75 mg 69238-1250-01 | Amneal | 100 capsules | — | AB | FDA listed | — |
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⏳ Availability & generic status
This product is an FDA-approved generic. Other versions of the same drug are listed under Therapeutic equivalents, least expensive first.
Where does this data come from?
📊 Medicare Part D spend CMS · PART D · 2026 (Q1)
📦 Packaging — all sizes for this product
| Package NDC | Description | Marketing start | Status |
|---|---|---|---|
| 43975-0315-10 You're viewing this | 100 CAPSULE, LIQUID FILLED in 1 BOTTLE (43975-315-10) | 2018-05-10 | Active |
🧭 About this NDC listing & data coverage
What data is (and isn’t) available for this NDC — tap to expand
| NDC identity (package / product / labeler codes) | ✓ Available |
| Labeler | ✓ Available |
| Product & package description | ✓ Available |
| Marketing category & status | ✓ Available |
| Active ingredient / dosage form / route | ✓ Available |
| FDA label (SPL via DailyMed) | ✓ Available |
| Package photos | — Not published for this NDC No photo available yet for this listing. |
| Inactive ingredients (structured) | — Not published for this NDC The labeler did not submit a structured excipient list, or no SPL is available. |
| NADAC pharmacy acquisition price (CMS) | — Not published for this NDC CMS publishes NADAC only for NDCs reported in its retail-pharmacy survey. |
| Orange Book / therapeutic-equivalence data | ✓ Available |
| HCPCS J-code billing crosswalk | — Not published for this NDC Most self-administered / retail products have no J-code — that is normal. |
| Medicaid utilization (CMS SDUD) | — Not published for this NDC CMS reports utilization only for NDCs with Medicaid claims above its privacy threshold. |
Questions about this listing
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📄 Full prescribing information FDA SPL
🚨 Boxed Warning ▾
WARNING: BIRTH DEFECTS Bexarotene is a member of the retinoid class of drugs that is associated with birth defects in humans. Bexarotene also caused birth defects when administered orally to pregnant rats. Bexarotene must not be administered to a pregnant woman.
( 8.1 ) WARNING: BIRTH DEFECTS See full prescribing information for complete boxed warning. Bexarotene is a member of the retinoid class of drugs that is associated with birth defects in humans. Bexarotene also caused birth defects when administered orally to pregnant rats.
Bexarotene must not be administered to a pregnant woman. ( 8.1 )
🎯 Indications and Usage ▾
1 INDICATIONS AND USAGE 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. Bexarotene capsules are 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 ▾
2 DOSAGE AND ADMINISTRATION The recommended initial dose of bexarotene capsules is 300 mg/m 2 /day (see Table 1). Bexarotene capsules 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: Bexarotene Capsules Initial Dose Calculation According to Body Surface Area Initial Dose Level (300 mg/m 2 /day) Number of 75 mg Bexarotene 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 bexarotene capsules 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 eight 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, bexarotene capsules were administered for up to 97 weeks.
Bexarotene capsules should be continued as long as the patient is deriving benefit. • Recommended initial dose is 300 mg/m 2 /day. ( 2 ) • Take bexarotene capsules 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 ▾
3 DOSAGE FORMS AND STRENGTHS Capsules: 75 mg, off-white, oblong soft gelatin capsules, imprinted “A78” with black ink. Capsules: 75 mg ( 3 )
⛔ Contraindications ▾
4 CONTRAINDICATIONS • Pregnancy (Boxed Warning, 4.1 ) • Known hypersensitivity to bexarotene ( 4.2 )
4.1Pregnancy Bexarotene can cause fetal harm when administered to a pregnant female. Bexarotene 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.
4.2Hypersensitivity Bexarotene capsules are contraindicated in patients with a known serious hypersensitivity to bexarotene or other components of the product.
⚠️ Warnings and Cautions ▾
5 WARNINGS AND PRECAUTIONS • Hyperlipidemia: Bexarotene capsules cause 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 bexarotene capsules and evaluate if suspected.
( 5.2 ) • Hepatotoxicity, cholestasis, and hepatic failure: Interrupt or discontinue bexarotene capsules and evaluate if liver chemistry tests exceed three times the upper limit of normal values. ( 5.3 ) • Hypothyroidism: Bexarotene capsule therapy can cause hypothyroidism. Monitor and replace thyroid hormone if needed ( 5.5 ) • Neutropenia: Monitor for neutropenia.
Reduce bexarotene capsule dose or interrupt as indicated. ( 5.6 ) • Photosensitivity: Minimize exposure to sunlight and artificial ultraviolet light during treatment. ( 5.10 )
5.1Hyperlipidemia Bexarotene 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 bexarotene capsules 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 bexarotene capsules. 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 bexarotene capsule therapy is initiated and weekly until the lipid response to bexarotene is established, which usually occurs within two to four weeks, and monitor at eight week intervals thereafter. Fasting triglycerides should be normal or normalized with appropriate intervention prior to initiating bexarotene capsule 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 bexarotene capsules. 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 bexarotene capsules [ see Drug Interactions (7) ].
5.2Pancreatitis Acute pancreatitis, including a fatal case, has been reported in four patients with CTCL and in six patients with non-CTCL cancers treated with bexarotene capsules; 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 bexarotene capsules 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 bexarotene capsules [ see Warnings and Precautions (5.1) ].
5.3Hepatotoxicity, cholestasis, and hepatic failure Bexarotene 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, w…
🤒 Adverse Reactions ▾
6 ADVERSE REACTIONS 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 ANI Pharmaceuticals, Inc. at 1-855-204-1431 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch.
6.1Clinical 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 bexarotene has been evaluated in two clinical trials of 152 patients with CTCL who received bexarotene capsules 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 bexarotene capsules 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 bexarotene capsule 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 bexarotene capsules (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 bexarotene capsules 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…
🔄 Drug Interactions ▾
7 DRUG INTERACTIONS Effect of Other Drugs on Bexarotene Capsules Gemfibrozil: Concomitant administration of bexarotene capsules and gemfibrozil resulted in increases in plasma concentrations of bexarotene. Concomitant administration of gemfibrozil with bexarotene capsules is not recommended. Effect of Bexarotene Capsules on Other Drugs Bexarotene 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 bexarotene capsules 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 bexarotene capsule therapy.
Drug Interactions Effect of Other Drugs on Bexarotene CYP3A4 Inhibitors/Inducers: In a clinical study, concomitant administration of multiple doses of ketoconazole with bexarotene capsules did not alter bexarotene plasma concentrations. This suggests that bexarotene elimination is not dependent on CYP3A4 metabolism. Paclitaxel plus Carboplatin: The co-administration of paclitaxel (200 mg/m 2 IV dose over 3 hours) plus carboplatin (at a dose expected to achieve an AUC of 6 mg●min/mL) with bexarotene capsules (400 mg/m 2 orally once daily) increased the exposure to bexarotene (AUC 0-24 and C max ) by 2-fold compared to bexarotene capsules alone.
Atorvastatin: Bexarotene concentrations were not affected by concomitant atorvastatin administration. Effect of Bexarotene on Other Drugs Bexarotene did not significantly inhibit the following enzymes in human liver microsomes: CYP1A2, CYP2A6, CYP2C9, CYP2C19, CYP2D6, CYP2E1 and CYP3A4. In vitro data suggested a potential for bexarotene to inhibit CYP2C8 and induce CYP3A4.
Atorvastatin: The exposure (AUC) to atorvastatin (a substrate for CYP3A4) decreased by half when atorvastatin was co-administered with bexarotene capsules (400 mg/m 2 orally once daily). Tamoxifen: Based on interim data, concomitant administration of bexarotene capsules and tamoxifen resulted in approximately a 35% decrease in plasma concentrations of tamoxifen, possibly through induction of CYP3A4 by bexarotene. Paclitaxel: The exposure (AUC) to paclitaxel (a substrate for CYP3A4 and CYP2C8) decreased by 19% when paclitaxel (200 mg/m 2 IV dose over 3 hours) was co-administered with bexarotene capsules (400 mg/m 2 orally once daily).
Carboplatin: The co-administration of bexarotene capsules (400 mg/m 2 orally once daily) had no effect on the exposure to free or total carboplatin.
👥 Use in Specific Populations ▾
8 USE IN SPECIFIC POPULATIONS
8.1Pregnancy Risk Summary Bexarotene, 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] . Bexarotene capsules must not be given to a pregnant female or a female who intends to become pregnant.
If pregnancy does occur during treatment with bexarotene capsules, 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 are 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).
8.2Lactation Risk Summary There is no information regarding the presence of bexarotene 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 bexarotene, discontinue breastfeeding during treatment with bexarotene capsules.
8.3Females 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 one week prior to bexarotene capsule therapy. Obtain another pregnancy test at monthly intervals while the patient remains on bexarotene capsules. Contraception Females Bexarotene 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 bexarotene is used. Effective contraception must be used for one month prior to the initiation of therapy, during therapy and for at least one 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 bexarotene capsules 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. Bexarotene capsule therapy should be initiated on the second or third day of a normal menstrual period. No more than a one month supply of bexarotene capsules 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 bexarotene capsules and for at least one month after the last dose of drug.
8.4Pediatric Use Safety and effectiveness of bexarotene in pediatric patients have not been established.
8.5Geriatric Use Of the total patients with CTCL in clinical trials of bexarotene capsules, 64% were 60 years or older, while 33% we…
🤰 Pregnancy ▾
8.1Pregnancy Risk Summary Bexarotene, 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] . Bexarotene capsules must not be given to a pregnant female or a female who intends to become pregnant.
If pregnancy does occur during treatment with bexarotene capsules, 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 are 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 ▾
8.4Pediatric Use Safety and effectiveness of bexarotene in pediatric patients have not been established.
🧓 Geriatric Use ▾
8.5Geriatric Use Of the total patients with CTCL in clinical trials of bexarotene capsules, 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 bexarotene capsules cannot be ruled out. Responses to bexarotene capsules were observed across all age group decades, without preference for any individual age group decade.
🆘 Overdosage ▾
10 OVERDOSAGE Doses up to 1000 mg/m 2 /day of bexarotene capsules 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.
🧬 Clinical Pharmacology ▾
12 CLINICAL PHARMACOLOGY
12.1Mechanism 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.
12.3Pharmacokinetics Terminal half-life of bexarotene is approximately seven hours. Studies in patients with advanced malignancies show approximate single dose linearity within the therapeutic range. Absorption After oral administration of bexarotene capsules, bexarotene is absorbed with a T max of about two hours.
Plasma bexarotene AUC and C max values resulting from a 75 to 300 mg dose were 35% and 48% higher, respectively, after a fat-containing meal than after a glucose solution. Distribution Bexarotene is highly bound (>99%) to plasma proteins. The plasma proteins to which bexarotene binds have not been elucidated, and the ability of bexarotene to displace drugs bound to plasma proteins and the ability of drugs to displace bexarotene capsules binding have not been studied.
Elimination Metabolism Four bexarotene metabolites have been identified in plasma: 6- and 7-hydroxy-bexarotene and 6- and 7-oxo-bexarotene. In vitro studies suggest that cytochrome P450 3A4 is the major cytochrome P450 responsible for formation of the oxidative metabolites and that the oxidative metabolites may be glucuronidated. The oxidative metabolites are active in in vitro assays of retinoid receptor activation, but the relative contribution of the parent and any metabolites to the efficacy and safety of bexarotene is unknown.
Excretion The renal elimination of bexarotene and its metabolites was examined in patients with Type 2 diabetes mellitus. Urinary elimination of bexarotene and its known metabolites is a minor excretory pathway (<1% of administered dose). Pharmacokinetics in Specific Populations Age: Based on the population pharmacokinetic analysis of data for 232 patients aged ≥65 years and 343 patients aged <65 years, age has no statistically significant effect on bexarotene pharmacokinetics.
Body Weight and Gender: Based on the population pharmacokinetics analysis of data for 614 patients with a weight range of 26 to 145 kg, the bexarotene apparent clearance increases with increasing body weight. Gender has no statistically significant effect on bexarotene pharmacokinetics. Race: Based on the population pharmacokinetic analysis of data for 540 Caucasian and 44 Black patients, bexarotene pharmacokinetics are similar in Blacks and Caucasians.
There are insufficient data to evaluate potential differences in the pharmacokinetics of bexarotene for other races. Renal Impairment: No formal studies have been conducted with bexarotene in patients with renal impairment. Urinary elimination of bexarotene and its known metabolites is a minor excretory pathway (<1% of administered dose), but because renal impairment can result in significant protein binding changes, pharmacokinetics may be altered in patients with renal impairment.
Hepatic Impairment: No specific studies have been conducted with bexarotene capsules in patients with hepatic impairment. Because less than 1% of the dose is excreted in the urine unchanged and there is in vitro evidence of extensive hepatic contribution to bexarotene elimination, hepatic impairment would be expected to lead to greatly decreased clearance. Drug Interactions Effect of Other Drugs on Bexarotene CYP3A4 Inhibitors/Inducers: In a clinical study, conc…
🧬 Mechanism of Action ▾
12.1Mechanism 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 / Storage and Handling ▾
16 HOW SUPPLIED/STORAGE AND HANDLING Bexarotene capsules are supplied as 75 mg off-white, opaque, oblong soft gelatin capsules, imprinted with black ink “A78”, in high density polyethylene bottles with child-resistant closures. Bottles of 100 capsules: NDC 43975-315-10 Store at 20° to 25°C (68° to 77°F) [see USP Controlled Room Temperature]. Avoid exposing to high temperatures and humidity after the bottle is opened. Protect from light.
📋 Description ▾
11 DESCRIPTION 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 bexarotene capsule contains 75 mg of bexarotene for oral administration. It also contains the following inactive ingredients: gelatin, nitrogen, butylated hydroxyanisole, glycerin, hydrolyzed gelatin, medium chain triglyceride, Shellac glaze, FD&C red #40, FD&C blue #1, FD&C yellow #6, propylene glycol, simethicone, polyethylene glycol 400, polysorbate 20, povidone, sorbitol, 1,4-sorbitan, mannitol, soy lecithin and titanium dioxide. structure
💬 Information for Patients ▾
17 PATIENT COUNSELING 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 bexarotene is contraindicated in pregnancy [ see Contraindications (4.1) ]. Bexarotene 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 bexarotene and for at least one month following discontinuation of therapy. • Advise females of reproductive potential of the importance of monthly pregnancy testing while taking bexarotene. • Advise females of reproductive potential to use effective contraception for one month prior to the initiation of therapy, during therapy, and for at least one 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 bexarotene capsule therapy should be initiated on the second or third day of a normal menstrual period. • Instruct patient to immediately stop taking bexarotene capsules 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 bexarotene capsules and for at least one 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) ]. Hepatotoxicit y 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 bexarotene [ 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 bexarotene capsule 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 bexarotene capsules 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 bexarotene capsules with a meal [ see Dosage and Administration (2) ].
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