temozolomide (Rx)

Brand and Other Names:Temodar
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Dosing & Uses

AdultPediatric

Dosage Forms & Strengths

capsule

  • 5mg
  • 20mg
  • 100mg
  • 140mg
  • 180mg
  • 250mg

powder for injection

  • 100mg/vial
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Anaplastic Astrocytoma

Indicated for the treatment of adults with refractory anaplastic astrocytoma (ie, patients with disease progression on a drug regimen containing nitrosourea and procarbazine)

Initial: 150 mg/m² PO/IV qDay for 5 days; repeat at 28-day cycles 

Maintenance: May increase/maintain dose at 200 mg/m² PO/IV qDay for 5 days/28-day cycle if ANC >1500 mm³ and platelets >100,000 mm³

Infuse IV over 90 minutes

Dosage modifications

  • Measure ANC and platelet on days 22 and 29 (day 1 of next cycle); modify dose for following cycle if:
  • ANC 1000-1500/mm³ or platelet 50,000-100,000/mm³: Postpone treatment until ANC >1500/mm³ and platelet >100,000/mm³; maintain initial dose
  • ANC <1000/mm³ or platelets <50,000/mm&sup3
    • Postpone therapy until ANC >1,500/mm³ and platelets >100,000/mm³
    • Decrease dose by 50 mg/m²/day for subsequent cycles
    • Do NOT administer drug at dose <100 mg/m² for anaplastic astrocytoma

Decrease maintenance dose

  • Reduce from 200 mg/m²/day to 150 mg/m²/day and from 150 mg/m²/day to 100 mg/m²/day if
    • ANC <10,000/mm³
    • Platelets <50,000/mm²
    • CTC Grade 3 nonhematologic toxicity

Glioblastoma Multiforme

Indicated for the treatment of adults with newly diagnosed glioblastoma multiforme concomitantly with radiotherapy and then as maintenance treatment

Initial: 75 mg/m² PO/IV qDay for 42 days concomitant with focal radiotherapy 

Infuse IV over 90 minutes

Continue treatment

  • Continue for up to 49 days if the criteria listed below are met
  • ANC ≥1,500/mm³, Platelet >100,000/mm³; CTC Grade 1 or lower

Dosage modifications (initial treatment and radiotherapy)

  • Interrupt if
    • ANC ≥500/mm³ but <1,500/mm³; CTC ≤Grade 1
    • Platelets: ≥10,000/mm³ but ≤100,000/mm³
    • CTC Grade 2 nonhematologic toxicity
  • Discontinue if
    • ANC <500/mm³
    • Platelets <10,000/mm³
    • CTC Grade 3 or 4 nonhematologic toxicity

Maintenance

  • Cycle 1 (Start 4 weeks AFTER temozolomide + radiotherapy): 150 mg/m² PO/IV qDay for 5 days, then 23-treatment free days
  • Cycle 2-6: may increase to 200 mg/m²/day if ANC >1500/mm³, platelets >100,000/mm³; CTC Grade <2

Newly Diagnosed High Grade Glioma (Orphan)

Orphan designation for treatment of newly diagnosed high grade glioma

Sponsor

  • Schering-Plough Research Institute; 2000 Galloping Hill Road; Kenilworth, NJ 07033

Advanced Metastatic Melanoma (Orphan)

Orphan designation for treatment of advanced metastatic melanoma

Sponsor

  • Schering-Plough Research Institute; 2000 Galloping Hill Road; Kenilworth, NJ 07033

Nasopharyngeal Carcinoma (Orphan)

(s)-perillyl alcohol temozolomide carbamate

Orphan designation for treatment of nasopharyngeal carcinoma

Sponsor

  • NeOnc Technologies, Inc; 8335 Sunset Blvd., #240; Los Angeles, California 90069

Glioblastoma Multiforme (Orphan)

Orphan designation for treatment of glioblastoma multiforme in pediatric patients

Sponsor

  • AmpliPharm Pharmaceuticals, LLC; 970 Peachtree Industrial Boulevard, Suite 100; Suwanee, Georgia 30024
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Interactions

Interaction Checker

and temozolomide

No Results

     activity indicator 
    No Interactions Found
    Interactions Found

    Contraindicated

      Serious - Use Alternative

        Significant - Monitor Closely

          Minor

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            Adverse Effects

            >10%

            Alopecia (55-69%)

            Lymphopenia (55%)

            Nausea (53%)

            Vomiting (42%)

            Headache (41%)

            Fatigue (34%)

            Constipation (33%)

            Anorexia (9-27%)

            Convulsions (23%)

            Thrombocytopenia (19%)

            Rash (8-19%)

            Hemiparesis (18%)

            Diarrhea (16%)

            Neutropenia (14%)

            Fever (13%)

            Asthenia (13%)

            Dizziness (12%)

            Peripheral edema (11%)

            Viral infections (11%)

            1-10% (selected)

            Amnesia (10%)

            Insomnia (10%)

            Abdominal pain (5-9%)

            Ataxia (8%)

            Back pain (8%)

            Paresis (8%)

            URI (8%)

            Urinary incontinence (8%)

            UTI (8%)

            Abnormal vision (5-8%)

            Pruritus (5-8%)

            Breast pain (6%)

            Depression (6%)

            Confusion (5%)

            Myalgia (5%)

            Weight gain (5%)

            Anemia (4%)

            Erythema (1%)

            Postmarketing Reports

            Alveolitis

            Interstitial pneumonitis

            Pulmonary fibrosis

            Hepatotoxicity including elevations of liver enzymes, hyperbillirubinemia, cholestasis, and hepatitis

            Diabetes insipidus

            Reactivation of infections including cytomegalovirus and hepatitis B

            Serious opportunistic infections, including some cases with fatal outcomes, can occur with bacterial, viral (primary and reactivated), fungal, and protozoan organisms

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            Warnings

            Contraindications

            Hypersensitivity to temozolomide, dacarbazine

            Cautions

            Myelosuppression reported, including prolonged pancytopenia; may result in aplastic anemia, which in some cases has resulted in a fatal outcome

            Severe hepatic/renal impairment, elderly

            Risk of myelodysplastic syndrome and secondary malignancies

            Prophylaxis for P. jiroveci pneumonia (pneumocystis pneumonia) required for all patients treated with temozolomide and radiation

            Obtain CBC prior to treatment on Day 1 and on Day 22 (21 days after the first dose) of each cycle; perform weekly if ANC declines

            Fatal and severe hepatotoxicity reported; perform LFTs at baseline, midway through the first cycle, prior to each subsequent cycle, and ~2-4 weeks after the last dose

            Causes fetal harm when administered to a pregnant women

            All patients, particularly those receiving steroids, should be observed closely for the development of lymphopenia and PCP

            As bioequivalence has been established only when given over 90 minutes, infusion over a shorter or longer period of time may result in suboptimal dosing; the possibility of an increase in infusion-related adverse reactions cannot be ruled out

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            Pregnancy & Lactation

            Pregnancy Category: D

            Lactation: Not known if excreted in breast milk, do not nurse

            Pregnancy Categories

            A:Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

            B:May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

            C:Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

            D:Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

            X:Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

            NA:Information not available.

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            Pharmacology

            Mechanism of Action

            Imidazotetrazine derivative prodrug; active metabolite MTIC methylates guanine-rich areas of DNA that initiate transcription, which lead to DNA double strand breaks and apoptosis

            Absorption

            Rapidly and completely absorbed after oral administration

            Peak Plasma Time: 1 hr (empty stomach); 2.25 hr (high-fat meal)

            Bioequivalence: 100%; IV infusion (when administered over 90 min) is bioequivalent to same dose of oral capsule

            Mean peak plasma concentration and AUC decreased by 32% and 9%, respectively when administered after a high-fat breakfast

            Distribution

            Protein Bound: 15%

            Vd: 0.4 L/kg

            Metabolism

            Metabolite: Hydrolyzed at physiologic pH to 3-methyl-(triazen-1-yl) imidazole-4-carboxamide (MTIC); MTIC further hydrolyzed to to 5-amino-imidazole-4-carboxamide (AIC), which is known to be an intermediate in purine and nucleic acid biosynthesis, and to methylhydrazine, which is believed to be the active alkylating species

            Elimination

            Half-life: 1.8 hr

            Clearance: 5.5 L/hr/m²

            Excretion: primarily urine (~38%)

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            Administration

            IV Preparation

            Bring the vial to room temp

            Reconstitute 100-mg vial with 41 mL SWI to obtain 2.5 mg/mL soln; gently swirl to dissolve (do not shake)

            After reconstitution, store at room temp and use within 14 hr, including infusion time

            Using aseptic technique, withdraw up to 40 mL per vial to get required dose and transfer into empty 250 mL PVC infusion bag

            IV Administration

            Infuse IV using pump over 90 min

            Flush lines before and after infusion

            Do not infuse other medications simultaneously thru same infusion line

            Oral Administration

            Take capsule consistently either with or without food; preferably take on empty stomach HS to avoid N/V

            May consider antiemetics before/after

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            Formulary

            FormularyPatient Discounts

            Adding plans allows you to compare formulary status to other drugs in the same class.

            To view formulary information first create a list of plans. Your list will be saved and can be edited at any time.

            Adding plans allows you to:

            • View the formulary and any restrictions for each plan.
            • Manage and view all your plans together – even plans in different states.
            • Compare formulary status to other drugs in the same class.
            • Access your plan list on any device – mobile or desktop.

            The above information is provided for general informational and educational purposes only. Individual plans may vary and formulary information changes. Contact the applicable plan provider for the most current information.

            Tier Description
            1 This drug is available at the lowest co-pay. Most commonly, these are generic drugs.
            2 This drug is available at a middle level co-pay. Most commonly, these are "preferred" (on formulary) brand drugs.
            3 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs.
            4 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            5 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            6 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            NC NOT COVERED – Drugs that are not covered by the plan.
            Code Definition
            PA Prior Authorization
            Drugs that require prior authorization. This restriction requires that specific clinical criteria be met prior to the approval of the prescription.
            QL Quantity Limits
            Drugs that have quantity limits associated with each prescription. This restriction typically limits the quantity of the drug that will be covered.
            ST Step Therapy
            Drugs that have step therapy associated with each prescription. This restriction typically requires that certain criteria be met prior to approval for the prescription.
            OR Other Restrictions
            Drugs that have restrictions other than prior authorization, quantity limits, and step therapy associated with each prescription.
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