pharmacopeia
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Boxed warning

ADRENAL CRISIS IN THE SETTING OF SHOCK, SEVERE TRAUMA OR INFECTION Patients treated with LYSODREN are at increased risk for developing adrenal crisis in the setting of shock, severe trauma or infection that may lead to death. If shock, severe trauma or infection occurs or develops, temporarily discontinue LYSODREN and administer exogenous steroids. Monitor patients closely for infections and instruct patients to contact their physician immediately if injury, infection, or any other concomitant illness occurs [see Dosage and Administration (2.3) and Warnings and Precautions (5.1)]. WARNING: ADRENAL CRISIS IN THE SETTING OF SHOCK, SEVERE TRAUMA OR INFECTION See full prescribing information for complete boxed warning. Patients treated with LYSODREN are at increased risk for developing adrenal crisis in the setting of shock, severe trauma or infection that may lead to death. If shock, severe trauma or infection occurs or develops, temporarily discontinue LYSODREN and administer exogenous steroids. Monitor patients closely for infections and instruct patients to contact their physician immediately if injury, infection, or any other concomitant illness occurs ( 2.3 , 5.1 ).

Mechanism of action

Sourced from openFDA

Mitotane is an adrenal cytotoxic agent with an unknown mechanism of action. Mitotane modifies the peripheral metabolism of steroids and directly suppresses the adrenal cortex.

Indications

Sourced from openFDA
  • LYSODREN is indicated for the treatment of patients with inoperable, functional or nonfunctional, adrenocortical carcinoma (ACC). LYSODREN is an adrenal cytotoxic agent indicated for the treatment of patients with inoperable, functional or nonfunctional, adrenocortical carcinoma (ACC).

Contraindications

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  • None. None.contraindicated

Dosage & administration

Sourced from openFDA

The recommended initial dose of LYSODREN is 2000 mg to 6000 mg orally, in three or four divided doses per day with food. ( 2.3 ) Titrate LYSODREN dose to achieve a plasma level of 14 to 20 mg/L. ( 2.3 ) LYSODREN is lipophilic and accumulates in adipose tissue. ( 2.3 ) 2.1 Recommended Evaluation and Testing Before Initiating LYSODREN Before initiating LYSODREN, evaluate pelvic ultrasound in premenopausal women, liver functions tests and complete blood count [see Warnings and Precautions (5.3 , 5.4 , 5.5) ]. 2.2 General Precautions LYSODREN is a hazardous drug. Advise caregivers to wear disposable gloves when handling LYSODREN tablets [see References (15) and Storage and Handling (16) ]. 2.3 Recommended Dosage and Administration Recommended Dosage The recommended initial dose of LYSODREN is 2000 mg to 6000 mg orally, in three or four divided doses per day. Monitor mitotane plasma levels and increase the dose based on patient tolerance and clinical response incrementally to achieve a mitotane plasma level of 14 to 20 mg/L, or as tolerated. Consider monitoring mitotane plasma levels every 2 weeks after starting treatment and after each dose adjustment. The target plasma level is usually reached within a period of 3 to 5 months. Monitor mitotane plasma levels periodically (e.g., monthly). Severe neurotoxicity may occur with levels > 20 mg/L. Dose Adjustments, Monitoring and Discontinuation In case of mitotane plasma levels above 20 mg/L without toxicities, consider reducing the dose by 50 to 75%.

Warnings & precautions

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Adrenal Insufficiency and Adrenal Crisis: Temporarily withhold LYSODREN during shock, trauma, infection or adrenal insufficiency. Steroid replacement may be necessary. (5.1) Central Nervous System (CNS) Toxicity : Monitor behavioral and neurologic assessments and mitotane plasma levels at regular intervals. Mitotane plasma levels exceeding 20 mg/L are associated with a greater incidence of toxicity. Advise patients not to drive or operate hazardous machinery if experiencing CNS adverse reactions. (5.2) Ovarian Macrocysts in Premenopausal Women : Monitor pelvic ultrasound at baseline and at regular intervals. Withhold, reduce the dose, or permanently discontinue LYSODREN based on severity. (5.3) Hepatotoxicity : Monitor liver functions tests prior to starting LYSODREN, during dose titration and as clinically indicated. Withhold, reduce the dose or permanently discontinue based on severity. (5.4) Hematologic Toxicity: Monitor complete blood counts prior to starting LYSODREN, during dose titration and as clinically indicated. Withhold, reduce the dose or permanently discontinue based on severity. (5.5) Prolonged Bleeding Time : Prolonged bleeding time has occurred in patients treated with mitotane and this should be taken into account when surgery is considered. (5.6) Embryo-Fetal Toxicity : Can cause fetal harm. Advise females of reproductive potential of the potential risk to a fetus and to use effective, nonhormonal contraception.

Adverse reactions

Sourced from openFDA

The following clinically significant adverse reactions are described elsewhere in the labeling: • Adrenal Insufficiency and Adrenal Crisis [see Warnings and Precautions (5.1)] • Central Nervous System Toxicity [see Warnings and Precautions (5.2)] • Ovarian Macrocysts in Premenopausal Women [see Warnings and Precautions (5.3)] • Hepatotoxicity [see Warnings and Precautions (5.4)] • Hematologic Toxicity [see Warnings and Precautions (5.5)] • Prolonged Bleeding Time [see Warnings and Precautions (5.6)] • Hormone Binding Protein [see Warnings and Precautions (5.7)] • Embryo-Fetal Toxicity [see Warnings and Precautions (5.8)] Most common adverse reactions include: anorexia, epigastric discomfort, nausea, vomiting, diarrhea, dizziness, vertigo, rash, hypercholesterolemia, hypertriglyceridemia, hypothyroidism, and decreased blood free testosterone in males. (6) To report SUSPECTED ADVERSE REACTIONS, contact Esteve Pharmaceuticals, S.A. at 1-888-306-6259 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.

Use in specific populations

Sourced from openFDA

8 USE IN SPECIFIC POPULATIONS Lactation :Advise not to breastfeed. (8.2) Hepatic Impairment :LYSODREN is not recommended for patients with severe hepatic impairment. In patients with mild to moderate hepatic impairment, monitor mitotane plasma levels frequently and modify the dosage as needed. (8.6) Renal Impairment : LYSODREN is not recommended for patients with severe renal impairment. In patients with mild or moderate renal impairment, monitor mitotane plasma levels frequently and modify the dosage as needed. (8.7) 8.1 Pregnancy Risk Summary LYSODREN can cause fetal harm. Limited postmarketing cases report preterm births and early pregnancy loss in women treated with LYSODREN during pregnancy. Animal reproduction studies have not been conducted with mitotane. Advise pregnant women of the potential risk to a fetus. In the U.S. general population, the estimated background risk of major birth defects and miscarriage in clinically recognized pregnancies is 2% to 4% and 15% to 20%, respectively. 8.2 Lactation Risk Summary Mitotane is excreted in human milk; however, the effect of LYSODREN on the breastfed child, or on milk production is unknown. Because of the potential for serious adverse reactions in a breastfed child, advise women not to breastfeed during treatment with LYSODREN and after discontinuation of treatment for as long as mitotane plasma levels are detectable.

Pharmacokinetics

Sourced from openFDA
Metabolism
Absorption Following oral administration of LYSODREN, 40% of the dose is absorbed. Effect of Food The effect of food on the absorption of mitotane (LYSODREN) is not known.

Overdosage

Sourced from openFDA

LYSODREN overdosage (plasma levels are above 20 mg/L) can cause central nervous system toxicity, including sedation, lethargy, and vertigo, as well as muscular weakness and gait disturbance. Withhold LYSODREN as clinically indicated for signs or symptoms of toxicity. LYSODREN is lipophilic and has a prolonged half-life; therefore, it may take weeks for plasma levels to decrease. LYSODREN is not likely to be dialyzable. Increase the frequency of mitotane plasma level monitoring, as clinically indicated.

Approval history

Sourced from openFDA
  • Jul 8, 1970NDANDA016885Esteve

FAERS reports

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Reference statistics only. FAERS reports are voluntarily submitted and are not incidence rates, safety signals, or causal evidence. Counts reflect reporting volume — how often a reaction was reported, not how often it occurs. For decision-grade use, consult openFDA and the FAERS Public Dashboard directly.
1,738 total reports matchedLatest report Share = reports listing the reaction ÷ total matched reports. Rows can sum to >100% because a single report often lists multiple reactions.
  1. 1Nausea28817%
  2. 2Off Label Use28817%
  3. 3Fatigue26615%
  4. 4Diarrhoea1609.2%
  5. 5Vomiting1488.5%
  6. 6Product Dose Omission Issue1307.5%
  7. 7Drug Ineffective1297.4%
  8. 8Adrenal Insufficiency1267.2%
  9. 9Decreased Appetite1136.5%
  10. 10Dizziness1126.4%
  11. 11Asthenia1046.0%
  12. 12Malignant Neoplasm Progression794.5%
  13. 13Death694.0%
  14. 14Drug Interaction694.0%
  15. 15Disease Progression673.9%

Literature

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Recent PubMed references pinned to Mitotane as a MeSH major topic. Citations link to pubmed.ncbi.nlm.nih.gov.

Clinical trials

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The 10 most recently updated of 23 ClinicalTrials.gov registrations naming Mitotane as an intervention. Registration is not evidence of efficacy or safety — reference crosswalk only.

Frequently asked questions

How does Mitotane work?
Mitotane is an adrenal cytotoxic agent with an unknown mechanism of action. Mitotane modifies the peripheral metabolism of steroids and directly suppresses the adrenal cortex.
What is Mitotane used for?
According to FDA labeling, Mitotane carries indications including: LYSODREN is indicated for the treatment of patients with inoperable, functional or nonfunctional, adrenocortical carcinoma (ACC). LYSODREN is an adrenal cytotoxic agent indicated for the treatment of patients with inoperable, functional or nonfunctional, adrenocortical carcinoma (ACC).. This is a reference summary of labeled uses, not medical advice or a treatment recommendation.
What class of drug is Mitotane?
Mitotane is classified as Other antineoplastic agents, Cytochrome P450 3A4 Inducers, Unknown Cellular or Molecular Interaction, Decreased Glucocorticoid Secretion.
What are the brand names for Mitotane?
Mitotane is marketed under brand names including Lysodren.
What are the contraindications for Mitotane?
Mitotane labeling lists contraindications including: None. None.. Always consult the full prescribing information and a clinician.
Note. Data for mitotane is illustrative MVP content compiled from public sources. pharmacopeia is for educational and informational use only and is not a substitute for professional medical advice.

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