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Targretin

Last reviewed on RxList: 7/15/2020
Targretin Side Effects Center

What Is Targretin?

Targretin (bexarotene) is a retinoid (vitamin A derivative) used to treat skin lesions of cutaneous T-cell lymphoma (CTCL) in patients who have not responded to or not tolerated other therapies.

What Are Side Effects of Targretin?

Common side effects of Targretin include:

  • headache
  • tiredness
  • fatigue
  • nausea
  • vomiting
  • dry skin
  • diarrhea
  • trouble sleeping
  • an increase in fats in the blood (blood lipids) such as cholesterol or triglycerides (blood tests will detect this)
  • an underactive thyroid (blood tests will detect this)
  • blood problems
  • weakness or loss of strength
  • swelling
  • rash, or
  • infections

Dosage for Targretin

The recommended initial dose of Targretin is 300 mg/m2/day, taken as a single oral daily dose with a meal.

What Drugs, Substances, or Supplements Interact with Targretin?

Vitamin A may increase side effects when taking Targretin. Limit vitamin A supplements to the recommended daily allowance (RDA) of 4000 to 5000 International Units (IU) a day. Check vitamin supplement labels for amounts of Vitamin A. Targretin may interact with gemfibrozil, ketoconazole, itraconazole, erythromycin, rifampin, phenobarbital, phenytoin, or diabetes medicine. Tell your doctor all medications and supplements you use.

Targretin During Pregnancy and Breastfeeding

Targretin must not be used during pregnancy. If you become pregnant or think you may be pregnant, inform your doctor. It is not known if this drug passes into breast milk. Due to possible harm to the nursing infant, breast-feeding while using this drug is not recommended.

Additional Information

Our Targretin (bexarotene) Side Effects Drug Center provides a comprehensive view of available drug information on the potential side effects when taking this medication.

This is not a complete list of side effects and others may occur. Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.

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Targretin Consumer Information

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Get emergency medical help if you have any signs of an allergic reaction: hives; difficult breathing; swelling of your face, lips, tongue, or throat.

Stop using bexarotene and call your doctor at once if you have:

  • blurred vision, eye pain, or seeing halos around lights;
  • low red blood cells (anemia)--pale skin, feeling light-headed or short of breath, rapid heart rate, trouble concentrating;
  • low white blood cell counts--fever, swollen gums, painful mouth sores, pain when swallowing, skin sores, cold or flu symptoms, cough, trouble breathing;
  • pancreatitis--severe pain in your upper stomach spreading to your back, nausea and vomiting; or
  • thyroid symptoms--extreme tired feeling, dry skin, joint pain or stiffness, muscle pain or weakness, hoarse voice, feeling more sensitive to cold temperatures, weight gain.

Common side effects may include:

  • headache, weakness;
  • nausea, stomach pain;
  • rash, dry skin; or
  • swelling in your hands or feet.

This is not a complete list of side effects and others may occur. Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.

Read the entire detailed patient monograph for Targretin (Bexarotene)

Targretin Professional Information

SIDE EFFECTS

The following serious adverse reactions are discussed in greater detail in other sections of the prescribing information:

  • Hyperlipidemia [see WARNINGS AND PRECAUTIONS]
  • Pancreatitis [see WARNINGS AND PRECAUTIONS]
  • Hepatotoxicity, Cholestasis, and Hepatic Failure [see WARNINGS AND PRECAUTIONS]
  • Hypothyroidism [see WARNINGS AND PRECAUTIONS]
  • Neutropenia [see WARNINGS AND PRECAUTIONS]
  • Cataracts [see WARNINGS AND PRECAUTIONS]
  • Vitamin A Supplementation Hazard [see WARNINGS AND PRECAUTIONS]
  • Hypoglycemia Risk in Patients with Diabetes Mellitus [see WARNINGS AND PRECAUTIONS]
  • Photosensitivity [see WARNINGS AND PRECAUTIONS]
  • Laboratory Tests [see WARNINGS AND PRECAUTIONS]
  • Drug/Laboratory Test Interactions [see WARNINGS AND PRECAUTIONS]

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/m2/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/m2/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/m2/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/m2/day than in patients treated at a starting dose of 300 mg/m2/day.

In patients with CTCL receiving an initial dose of 300 mg/m2/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/m2/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/m2/day to 1000 mg/m2/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/m2/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.

Table 2: Adverse Events with Incidence ≥10% in CTCL Trials

Initial Assigned Dose Group
(mg/m2/day)
300>300
Body SystemN=84N=53
Adverse Event (AE)*,N (%)N (%)
METABOLIC AND NUTRITIONAL DISORDERS
Hyperlipemia66 (79)42 (79)
Hypercholesteremia27 (32)33 (62)
Lactic dehydrogenase increased6 (7)7 (13)
BODY AS A WHOLE
Headache25 (30)22 (42)
Asthenia17 (20)24 (45)
Infection11 (13)12 (23)
Abdominal pain9 (11)2 (4)
Chills8 (10)7 (13)
Fever4 (5)9 (17)
Flu syndrome3 (4)7 (13)
Back pain2 (2)6 (11)
Infection bacterial1 (1)7 (13)
ENDOCRINE
Hypothyroidism24 (29)28 (53)
SKIN AND APPENDAGES
Rash14 (17)12 (23)
Dry skin9 (17)5 (9)
Exfoliative dermatitis8 (10)15 (28)
Alopecia3 (4)6 (11)
HEMIC AND LYMPHATIC SYSTEM
Leukopenia14 (17)25 (47)
Anemia5 (6)13 (25)
Hypochromic anemia3 (4)7 (13)
DIGESTIVE SYSTEM
Nausea13 (16)4 (8)
Diarrhea6 (7)22 (42)
Vomiting3 (4)7 (13)
Anorexia2 (2)12 (23)
CARDIOVASCULAR SYSTEM
Peripheral edema11 (13)6 (11)
NERVOUS SYSTEM
Insomnia4 (5)6 (11)
* Preferred English term coded according to Ligand-modified COSTART 5 Dictionary.
Patients are counted at most once in each AE category.

Table 3: Incidence of Moderately Severe and Severe Adverse Events Reported in at Least Two Patients (CTCL Trials)

Reported in at Least Two Patients (CTCL Trials)Initial Assigned Dose Group (mg/m2/day)
300 (N=84)>300 (N=53)
Mod SevSevereMod SevSevere
Body System
Adverse Event (AE)*,N (%)N (%)N (%)N (%)
BODY AS A WHOLE
Asthenia1 (1)0 (0)11 (21)0 (0)
Headache3 (4)0 (0)5 (9)1 (2)
Infection bacterial1 (1)0 (0)0 (0)2 (4)
CARDIOVASCULAR SYSTEM
Peripheral edema2 (2)1 (1)0 (0)0 (0)
DIGESTIVE SYSTEM
Anorexia0 (0)0 (0)3 (6)0 (0)
Diarrhea1 (1)1 (1)2 (4)1 (2)
Pancreatitis1 (1)0 (0)3 (6)0 (0)
Vomiting0 (0)0 (0)2 (4)0 (0)
ENDOCRINE
Hypothyroidism1 (1)1 (1)2 (4)0 (0)
HEMIC AND LYMPHATIC SYSTEM
Leukopenia3 (4)0 (0)6 (11)1 (2)
METABOLIC AND NUTRITIONAL DISORDERS
Bilirubinemia0 (0)1 (1)2 (4)0 (0)
Hypercholesteremia2 (2)0 (0)5 (9)0 (0)
Hyperlipemia16 (19)6 (7)17 (32)5 (9)
SGOT/AST increased0 (0)0 (0)2 (4)0 (0)
SGPT/ALT increased0 (0)0 (0)2 (4)0 (0)
RESPIRATORY SYSTEM
Pneumonia0 (0)0 (0)2 (4)2 (4)
SKIN AND APPENDAGES
Exfoliative dermatitis0 (0)1 (1)3 (6)1 (2)
Rash1 (1)2 (2)1 (2)0 (0)
* Preferred English term coded according to Ligand-modified COSTART 5 Dictionary.
Patients are counted at most once in each AE category. Patients are classified by the highest severity within each row.

Table 4: Treatment-Emergent Abnormal Laboratory Values in CTCL Trials

Initial Assigned Dose (mg/m2/day)
300>300
N=83*N=53*
AnalyteGrade 3
(%)
Grade 4
(%)
Grade 3
(%)
Grade 4
(%)
Triglycerides2173214
Total cholesterol1971630
Alkaline phosphatase1002
Hyperglycemia1060
Hypocalcemia1000
Hyponatremia1090
SGPT/ALT1022
Hyperkalemia0020
Hypernatremia0100
SGOT/AST0022
Total bilirubin0002
ANC decreased124198
ALC decreased70150
WBC decreased40110
Hemoglobin decreased0020
* Number of patients with at least one analyte value post-baseline.
Adapted from NCI Common Toxicity Criteria, Grade 3 and 4, Version 2.0. Patients are considered to have had a Grade 3 or 4 value if either of the following occurred: a) Value becomes Grade 3 or 4 during the study; b) Value is abnormal at baseline and worsens to Grade 3 or 4 on study, including all values beyond study drug discontinuation, as defined in data handling conventions.
The denominator used to calculate the incidence rates for fasting Total Cholesterol and Triglycerides were N=75 for the 300 mg/m2/day initial dose group and N=44 for the >300 mg/m2/day initial dose group.

The safety profile from the one post-approval trial with 59 subjects was generally comparable to that of the pivotal trials with the exception of serious adverse events hypertriglyceridemia, neutropenia and bone marrow failure which were observed more frequently in the TARGRETIN 300 mg/m2/day group than in the TARGRETIN 150 mg/m2/day group.

Severe hypertriglyceridemia (≥800 mg/dL) was not seen in any subject in the lower dosage arm.

The most common AEs by preferred term in either the TARGRETIN 300 or 150 mg/m2/day treatment group were as follows: hypertriglyceridemia (18 subjects [62.1%] and 17 subjects [56.7%], respectively); hypothyroidism (15 subjects [51.7%] and 13 subjects [43.3%], respectively); headache (9 subjects [31.0%] and 7 subjects [23.3%], respectively); hypercholesterolemia (8 subjects [27.6%] and 7 subjects [23.3%], respectively); neutropenia (7 subjects [24.1%] and 2 subjects [6.7%], respectively); and skin exfoliation (5 subjects [17.2%] and 5 subjects [16.7%], respectively).

Higher percentage of subjects in the TARGRETIN 300 mg/m2/day group than in the TARGRETIN 150 mg/m2/day group experienced SAEs (13 subjects [44.8%] vs 11 subjects [36.7%], respectively.

Of the SAEs of special interest, there were more events in the TARGRETIN 300 mg/m2/day group than in TARGRETIN 150 mg/m2/day group of bone marrow failure (3 [10.3%] vs 1 [3.3%, respectively]), neutropenia (3 [10.3%] vs 0 [0%], respectively), and hypertriglyceridemia (9 [31%] vs 2 [6.7%], respectively).

Read the entire FDA prescribing information for Targretin (Bexarotene)

Related Resources for Targretin

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Read the Targretin User Reviews »

© Targretin Patient Information is supplied by Cerner Multum, Inc. and Targretin Consumer information is supplied by First Databank, Inc., used under license and subject to their respective copyrights.

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