What is temozolomide used to treat?
Drug type: Temozolomide is an anti-cancer ("antineoplastic" or "cytotoxic") chemotherapy drug. This medication is classified as an "alkylating agent." (For more detail, see "How this drug works" section below). Treatment of anaplastic astrocytoma, glioblastoma multiforme (GBM) (types of brain tumors).
How often should you take temozolomide?
Take temozolomide at around the same time every day. For some types of brain tumors, temozolomide is taken daily for 42–49 days. Then, after a 28-day break, it may be taken once a day for 5 days in a row, followed by a 23-day break before repeating the next dosage cycle.
What are the results of the temozolomide trial?
Trials Produce Practice-Changing Results for Brain Cancer. A pivotal 2005 trial showed that temozolomide can improve how long patients with glioblastoma live. The trial, however, was restricted to patients younger than 70, and very few patients over age 65 were included in the trial, he said.
What are the side effects of temozolomide capsules?
Temozolomide capsules, USP can affect your bone marrow and cause you to have decreased blood cell counts. Decreased white blood cell count, red blood cell count and platelet count are common with Temozolomide capsules, USP but it can also be severe and lead to death.
What does temozolomide treat?
Temozolomide is used to treat specific types of brain cancer (eg, glioblastoma multiforme, anaplastic astrocytoma) in patients whose tumors have returned or whose tumors have just been diagnosed. It belongs to the group of medicines known as antineoplastics (cancer medicines).
Why is temozolomide important?
Temozolomide works by stopping cancer cells from making DNA. DNA stands for DeoxyriboNucleic Acid. It is the genetic material of a cell. If the cancer cells can't make DNA, they can't split into 2 new cells, so the cancer can't grow.
What type of chemotherapy is temozolomide?
Drug type: Temozolomide is an anti-cancer ("antineoplastic" or "cytotoxic") chemotherapy drug. This medication is classified as an "alkylating agent." (For more detail, see "How this drug works" section below).
How does temozolomide target cancer cells?
Summary. Temozolomide is a monofunctional alkylating agent with established utility in the treatment of malignant glioma. This chemotherapy induces cytotoxic damage through the creation of methyl adducts at the O6 position on the DNA base guanine.
How effective is temozolomide?
Whole brain radiation therapy (WBRT) and temozolomide can be efficacious, with a complete response rate of 85% in one small study.
Why is temozolomide used for glioblastoma?
The addition of temozolomide regimen improved the overall survival and progression-free survival in patients with GBM compared with radiotherapy alone. Temozolomide is a lipophilic molecule that crosses the blood-brain barrier and is stable at the acidic pH of the stomach and is therefore administered orally.
What is Temodar used for?
Temodar (temozolomide) This chemotherapy medication is given for a variety of brain tumors types, primarily gliomas. It may be prescribed at a lower dose for daily use during radiation therapy or at a higher dose when used for only five days per month.
When do you take temozolomide?
Temozolomide comes as a capsule to take by mouth. It is usually taken once a day in the evening at bedtime. Take temozolomide capsules on an empty stomach with a glass of water. Take temozolomide at around the same time every day.
What is temozolomide made of?
Temozolomide is a prodrug; it is spontaneously hydrolyzed at physiological pH to 3-methyl-(triazen-1-yl)imidazole-4-carboxamide (MTIC), which further splits into monomethylhydrazine, likely the active methylating agent, and 5-aminoimidazole-4-carboxamide (AIC).
Is temozolomide targeted therapy?
Temozolomide as a targeted therapy strategy for triple negative breast cancer [abstract].
How is temozolomide excreted?
Temozolomide and its metabolites are excreted via the kidneys. Nausea and vomiting are common side effects and are usually mild to moderate. Seizure and thrombocytopenia are noted in less than 7% of patients.
Does temozolomide cross the blood brain barrier?
TMZ is 100% bioavailable when taken orally and, because of its small size and lipophilic properties, it is able to cross the blood-brain barrier. Concentrations in the central nervous system are approximately 30% of plasma concentrations.
Usual Adult Dose for Anaplastic Astrocytoma
Oral: Initial Dose: 150 mg/m2 orally once a day Maintenance Dose: 200 mg/m2 orally once a day Duration of Therapy: 5 consecutive days per 28-day treatment cycle IV: Initial Dose: 150 mg/m2 IV over 90 minutes once a day Maintenance Dose: 200 mg/m2 IV over 90 minutes once a day Duration of Therapy: 5 consecutive days per 28-day treatment cycle Comments: -Dose should only be increased to 200 mg/m2 if both the nadir and day of dosing (Day 29, Day 1 of next cycle), the ANC is greater than or equal to 1.5 x 10 (9)/L and platelet count is greater than or equal to 100 x 10 (9)/L. -A complete blood count should be obtained on day 22 or within 48 hours of that day of each cycle and weekly until the ANC is above 1.5 x 10 (9)/L and the platelet count is above 100 x 10 (9)/L. -The next cycle should not be started until the ANC and platelet count exceed the above levels. -In clinical trial, treatment could be continued for a maximum of 2 years.
Usual Adult Dose for Glioblastoma Multiforme
Concomitant phase with focal radiotherapy: Oral: 75 mg/m2 orally once a day Duration of therapy: 42 days IV: 75 mg/m2 IV over 90 minutes once a day Duration of therapy: 42 days Comments: -No dose reductions are recommended during the concomitant phase. -Dose interruptions or discontinuation may occur based on toxicity. -Therapy should continue throughout the 42-day concomitant phase up to 49 days if all of the following conditions are met: ANC greater than or equal to 1.5 x 10 (9)/L, platelet count greater than 100 x 10 (9)/L, common toxicity criteria (CTC) nonhematological toxicity less than or equal to Grade 1. -A complete blood count should be obtained weekly during treatment. -Pneumocystis pneumonia prophylaxis is required during the concomitant administration of this drug and radiotherapy, and should be continued in patients who develop lymphocytopenia until recovery. Monotherapy Phase: Cycle 1: Oral: 150 mg/m2 orally once a day Duration of therapy: 5 days followed by 23 days without treatment IV: 150 mg/m2 IV over 90 minutes once a day Duration of therapy: 5 days followed by 23 days without treatment Cycles 2-6: Oral: 200 mg/m2 by mouth once a day Duration of therapy: First 5 days of each cycle IV: 200 mg/m2 IV over 90 minutes once a day Duration of therapy: First 5 days of each cycle Comments: -At the start of cycle 2, the dose should be escalated to 200 mg/m2 if: CTC nonhematological toxicity for Cycle 1 is grade less than or equal to 2 (except for alopecia, nausea, and vomiting), ANC is greater than or equal to 1.5 x 10 (9)/L, and the platelet count is greater than or equal to 100 x 10 (9)/L. -The dose remains at 200 mg/m2 for cycles 2 through 6 unless toxicity occurs. -If the dose was not escalated at the beginning of cycle 2, escalation should not be done in subsequent cycles. -Obtain a complete blood count on day 22 or within 48 hours of that day of each cycle and weekly until the ANC is greater than 1.5 x 10 (9)/L and the platelet count is greater than 100 x 10 (9)/L.
Usual Pediatric Dose for Anaplastic Astrocytoma
Less than 3 years: Safety and efficacy have not been established 3 years or older: Previously Untreated with Chemotherapy: 200 mg/m2 orally once a day Duration of therapy: 5 days followed by 23 days without treatment Previously Treated with Chemotherapy: Initial Dose: 150 mg/m2 orally once a day Maintenance Dose: 200 mg/m2 orally once a day Duration of therapy: First 5 days of each treatment cycle Comments: -Dose in cycle 2 for patients previously treated with chemotherapy should be increased if there is no haematological toxicity. -If the nadir on day of dosing (Day 29, Day 1 of next cycle) absolute neutrophil counts (ANC) are greater than or equal to 1.5 × 10 (9)/L and platelet counts are greater than or equal to 100 × 10 (9)/L, the dose may be increased to 200 mg/m2 orally once daily for 5 consecutive days per 28 day treatment cycle. -During treatment, a complete blood count should be obtained on Day 22 (21 days after the first dose) or within 48 hours of that day, and weekly until the ANC is above 1.5 × 10 (9)/L and the platelet count exceeds 100 × 10 (9)/L.
Usual Pediatric Dose for Glioblastoma Multiforme
Less than 3 years: Safety and efficacy have not been established 3 years or older: Previously Untreated with Chemotherapy: 200 mg/m2 orally once a day Duration of therapy: 5 days followed by 23 days without treatment Previously Treated with Chemotherapy: Initial Dose: 150 mg/m2 orally once a day Maintenance Dose: 200 mg/m2 orally once a day Duration of therapy: First 5 days of each treatment cycle Comments: -Dose in cycle 2 for patients previously treated with chemotherapy should be increased if there is no haematological toxicity. -If the nadir on day of dosing (Day 29, Day 1 of next cycle) absolute neutrophil counts (ANC) are greater than or equal to 1.5 × 10 (9)/L and platelet counts are greater than or equal to 100 × 10 (9)/L, the dose may be increased to 200 mg/m2 orally once daily for 5 consecutive days per 28 day treatment cycle. -During treatment, a complete blood count should be obtained on Day 22 (21 days after the first dose) or within 48 hours of that day, and weekly until the ANC is above 1.5 × 10 (9)/L and the platelet count exceeds 100 × 10 (9)/L.
Renal Dose Adjustments
Dose adjustment (s) may be required in patients; however, no specific guidelines have been suggested. Caution is recommended.
Liver Dose Adjustments
Dose adjustment (s) may be required; however, no specific guidelines have been suggested. Caution is recommended.
Dose Adjustments
Glioblastoma Multiforme: Concomitant Phase: Interruption of Therapy: -Absolute Neutrophil Count (ANC) greater than or equal to 0.5 and less than 1.5 x 10 (9)/L -Platelet count greater than or equal to 10 and less than 100 x 10 (9)/L -Common Toxicity Criteria (CTC) Nonhematological Toxicity (except for alopecia, nausea, vomiting) grade 2 Discontinuation of Therapy: -ANC less than 0.5 x 10 (9)/L -Platelet count less than 10 x 10 (9)/L -CTC Nonhematological Toxicity grade 3 or 4 Maintenance Phase: Reduce Dose by 1 Dose Level: -Dose should be reduced to 100 mg/m2 for prior toxicity -ANC less than 1.0 x 10 (9)/L -Platelet count less than 50 x 10 (9)/L -CTC Nonhematological Toxicity grade 3 Discontinuation of Therapy: -If dose reduction to less than 100 mg/m2 is required. -If the same Grade 3 CTC nonhematological toxicity recurs after dose reduction. -CTC Nonhematological Toxicity grade 4 Anaplastic Astrocytoma: Dose Reduction: -If the ANC falls below 1.0 x 10 (9)/L or the platelet count is less than 50 x 10 (9)/L during any cycle, the next cycle should be reduced by 50 mg/m2 but not below 100 mg/m2..
How long does temozolomide last?
Median overall survival in patients treated with both radiation and temozolomide was 9.3 months, compared with 7.6 months in patients who received radiation therapy alone. The radiation and temozolomide combination also modestly improved progression-free survival.
What age group is the glioblastoma trial?
The trial, led by the Canadian Cancer Trials Group (CCTG), focused on patients over the age of 65.
Can temozolomide be given to glioblastoma patients?
Given the survival advantages seen when temozolomide is given to patients with glioblastoma, some oncologists already offer it to their patients with anaplastic glioma , explained Brian Alexander, M.D., of the Center for Neuro-Oncology at the Dana-Farber Cancer Institute. From the perspective of potential side effects, ...
How long does temozolomide last?
Temozolomide is usually taken at home. Typical duration of therapy with radiation is six weeks. Click here for common starting doses .
Why is temozolomide used for brain cancer?
Temozolomide with radiation is not commonly given with the goal of cure, but can decrease symptoms from glioblastoma brain cancer and prolong life.
How long before a meal should I take anti nausea medication?
Of the ones you have been given, ask your nurse or pharmacist for guidance which to take and when. If you are having difficulty eating, anti-nausea medications taken 30 to 60 minutes before a meal can sometimes help.
Why do some medications need to be stopped?
Some medications need to be stopped or changed before starting treatment because they may not be needed . On occasion, other medications may need to be switched to a different one, or stopped altogether if they interact with new anti-cancer medications or supportive care medications that are prescribed for you.
What labs are needed for MGMT?
Labs (blood tests) may be checked before treatment and weekly during treatment. Labs often include: Complete Blood Count (CBC), Comprehensive Metabolic Panel (CMP), plus any others your doctor may order. A small sample of brain tissue may be analyzed to see how the MGMT gene is functioning.
Does temozolomide cause nausea?
In clinical studies, the most commonly reported side effects with temozolomide with radiation are shown here: Note: Nausea, vomiting, and constipation may be more common in patients older than 65 years. On average, 5% of patients discontinued temozolomide due to unacceptable side effects.
How many cycles of temozolomide?
You can have up to 12 cycles of treatment with temozolomide. A cycle of treatment means that you take temozolomide for some days and then have a break to allow your body to recover.
How often can you take temozolomide?
Temozolomide with radiotherapy. You usually take temozolomide once a day for between 6 to 7 weeks. You also have radiotherapy every day, Monday to Friday, during this time. Your doctor will tell you how many radiotherapy treatments you’ll have in total.
What do they check before and during a chemo treatment?
You have blood tests before and during your treatment. They check your levels of blood cells and other substances in the blood. They also check how well your liver and kidneys are working.
How long can you stay off live shots?
Don’t have immunisations with live vaccines while you’re having treatment and for up to 12 months afterwards. The length of time depends on the treatment you are having. Ask your doctor or pharmacist how long you should avoid live vaccinations.
How long should TMZ be taken?
It should be swallowed whole. If you’ve been newly diagnosed with a glioblastoma, a typical treatment would be radiotherapy for up to 6 weeks, alongside TMZ taken orally every day. It should preferably be taken at the same time each day. This initial period is known as the concomitant phase.
How often does a TMZ oncologist monitor you?
During this phase, your oncologist will monitor you weekly. Your general health will be monitored along with regular tests, for example full blood counts or bone marrow function. The results will then be used to decide whether you should continue to take TMZ as part of your treatment.
What is TMZ used for?
Temozolomide. Temozolomide (TMZ) is a chemotherapy drug that has been shown to improve average survival rate for people with some high grade brain tumours. Temozolomide (pronounced tee-mo-zol-oh-m-ide) is a type of chemotherapy drug that's approved for the treatment of glioblastomas and anaplastic astrocytomas.
Can TMZ be prescribed for gliomas?
During this phase, blood counts will be taken once on the last day of each cycle. TMZ might also be prescribed on its own for adults or children with high grade gliomas as a second line of treatment. This means if the tumour has not responded to other standard treatment, or if the tumour comes back - known as recurrence.
Is TMZ a chemo drug?
As a result, it's the main chemotherapy drug used globally for the treatment of glioblastoma. Although TMZ, like all chemotherapy drugs, may cause some side-effects, the clinical trials have shown that the possible benefits when treating high grade gliomas far outweigh the risks.
Can TMZ be resistant to DNA?
In some cases, tumour cells can become resistant to the effect of TMZ. Research funded by The Brain Tumour Charity found that tumour cells containing more of a protein involved in DNA repair (known by the letters MGMT) are able to repair themselves and make the TMZ less effective. At present, only a biopsy sample of the tumour can reveal ...
Is Temodar the same as TMZ?
Temodal® and Temodar® are brand names of the same drug. Large-scale clinical trials have shown that TMZ, when given alongside radiotherapy, improves average survival for people with high grade tumours, compared to those who only have radiotherapy. As a result, it's the main chemotherapy drug used globally for the treatment of glioblastoma.
What is temozolomide used for?
Expand Section. Temozolomide is used to treat certain types of brain tumors. Temozolomide is in a class of medications called alkylating agents. It works by slowing or stopping the growth of cancer cells in your body.
What are the side effects of temozolomide?
Temozolomide may cause side effects. Tell your doctor if any of these symptoms are severe or do not go away: 1 nausea 2 vomiting 3 diarrhea 4 constipation 5 loss of appetite 6 sores in the mouth and throat 7 headache 8 pale skin 9 lack of energy 10 loss of balance or coordination 11 fainting 12 dizziness 13 hair loss 14 insomnia 15 memory problems 16 changes in vision
How often should I take temozolomide?
It is usually taken once a day in the evening at bedtime. Take temozolomide capsules on an empty stomach with a glass of water. Take temozolomide at around the same time every day. For some types of brain tumors, temozolomide is taken daily for 42–49 days. Then, after a 28-day break, it may be taken once a day for 5 days in a row, ...
What to do if you are allergic to temozolomide?
Before taking temozolomide, tell your doctor and pharmacist if you are allergic to temozolomide, dacarbazine (DTIC-Dome) any other medications, or any of the ingredients in temozolomide capsules. Ask your pharmacist for a list of the ingredients. tell your doctor and pharmacist what other prescription and nonprescription medications, vitamins, ...
What to do if your capsules are broken?
If any of the capsules are broken or leaking, do not touch them with your bare hands and be careful not to breathe in the powder from the capsules. You should wear rubber or latex gloves when you handle broken or opened capsules so that your skin does not come into contact with the powder.
What is the phone number to call for poison control?
In case of overdose, call the poison control helpline at 1-800-222-1222. Information is also available online at https://www.poisonhelp.org/help. If the victim has collapsed, had a seizure, has trouble breathing, or can't be awakened, immediately call emergency services at 911.
Can you take more than one temozolomide?
Take temozolomide exactly as directed. Do not take more or less of it or take it more often than prescribed by your doctor. Your full dose may contain more than one type and color of capsules and may be contained in more than one prescription bottle.
What is the generic name for temozolomide?
Chemocare.com uses generic names in all descriptions of drugs. Temodar is the trade name for temozolomide. In some cases, health care professionals may use the trade name temodar when referring to the generic drug name temozolomide.
Can you take aspirin with temozolomide?
Do not take aspirin, or products containing aspirin unless your doctor specifically permits this.
Indications and Usage
- Newly Diagnosed Glioblastoma
Temozolomide capsules, USP is indicated for the treatment of adult patients with newly diagnosed glioblastoma concomitantly with radiotherapy and then as maintenance treatment. - Refractory Anaplastic Astrocytoma
Temozolomide capsules, USP is indicated for the treatment of adult patients with refractory anaplastic astrocytoma who have experienced disease progression on a drug regimen containing nitrosourea and procarbazine.
Dosage and Administration
- Recommended Dosage and Dosage Modifications for Newly Diagnosed Glioblastoma
Administer Temozolomide capsules, USP orally once daily for 42 consecutive days during the concomitant phase with focal radiotherapy and then once daily on Days 1 to 5 of each 28-day cycle for 6 cycles during the maintenance phase. Provide Pneumocystis pneumonia (PCP) prop… - Recommended Dosage and Dosage Modifications for Refractory Anaplastic Astrocytoma
The recommended initial dosage of Temozolomide is 150 mg/m2 once daily on Days 1 to 5 of each 28-day cycle. Increase the Temozolomide dose to 200 mg/m2per day if the following conditions are met at the nadir and on Day 1 of the next cycle: 1. ANC is greater than or equal to …
Contraindications
- Temozolomide capsules, USP is contraindicated in patients with a history of hypersensitivity reactions to: 1. Temozolomide or any other ingredients in Temozolomide capsules, USP; and 2. dacarbazine, since both Temozolomide and dacarbazine are metabolized to the same active metabolite 5-(3-methyltriazen-1-yl)-imidazole-4-carboxamide. Reactions to Temozolomide have i…
Warnings and Precautions
- Myelosuppression
Myelosuppression, including pancytopenia, leukopenia and anemia, some with fatal outcomes, have occurred with Temozolomide [see Adverse Reactions (6.1, 6.2)].Geriatric patients and women have been shown in clinical trials to have a higher risk of developing myelosuppression. … - Myelodysplastic Syndrome and Secondary Malignancies
Cases of myelodysplastic syndrome and secondary malignancies, including myeloid leukemia, have been observed following Temozolomide administration.
Adverse Reactions
- The following clinically significant adverse reactions are described elsewhere in the labeling: 1. Myelosuppression [see Warnings and Precautions (5.1)]. 2. Myelodysplastic Syndrome and Secondary Malignancies [see Warnings and Precautions (5.2)]. 3. Pneumocystis Pneumonia [see Warnings and Precautions (5.3)]. 4. Hepatotoxicity [see Warnings and Precautions (5.4)].
Use in Specific Populations
- Pregnancy
Risk Summary Based on its mechanism of action [see Clinical Pharmacology (12.1)] and findings from animal studies, Temozolomide can cause fetal harm when administered to a pregnant woman. Available postmarketing reports describe cases of spontaneous abortions and congenit… - Lactation
There are no data on the presence of Temozolomide or its metabolites in human milk, the effects on a breastfed child, or the effects on milk production. Because of the potential for serious adverse reactions, including myelosuppression from Temozolomide in the breastfed children, ad…
Overdosage
- Dose-limiting toxicity was myelosuppression and was reported with any dose but is expected to be more severe at higher doses. An overdose of 2000 mg per day for 5 days was taken by one patient and the adverse reactions reported were pancytopenia, pyrexia, multi-organ failure, and death. There are reports of patients who have taken more than 5 days of treatment (up to 64 day…
Temozolomide Description
- Temozolomide is an alkylating drug. The chemical name of Temozolomide is 3,4-dihydro-3-methyl-4-oxoimidazo[5,1-d]-as-tetrazine-8-carboxamide. The structural formula of Temozolomide is: The material is a white to light tan/light pink powder with a molecular formula of C6H6N6O2 and a molecular weight of 194.15. The molecule is stable at acidic pH (<5) and labile at pH >7; h…
Temozolomide - Clinical Pharmacology
- Mechanism of Action
Temozolomide is not directly active but undergoes rapid nonenzymatic conversion at physiologic pH to the reactive compound 5-(3-methyltriazen-1-yl)-imidazole-4-carboxamide (MTIC). The cytotoxicity of MTIC is thought to be primarily due to alkylation of DNA. Alkylation (methylation) … - Pharmacokinetics
Following a single oral dose of 150 mg/m2, the mean Cmax value for Temozolomide was 7.5 mcg/mL and for MTIC was 282 ng/mL. The mean AUC value for Temozolomide was 23.4 mcg·hr/mL and for MTIC was 864 ng·hr/mL. Temozolomide exhibits linear kinetics over the ther…
Nonclinical Toxicology
- Carcinogenesis, Mutagenesis, Impairment of Fertility
Temozolomide is carcinogenic in rats at doses less than the maximum recommended human dose. Temozolomide induced mammary carcinomas in both males and females at doses 0.13 to 0.63 times the maximum human dose (25-125 mg/m2) when administered orally on 5 consecuti… - Animal Toxicology and/or Pharmacology
Toxicology studies in rats and dogs identified a low incidence of hemorrhage, degeneration, and necrosis of the retina at Temozolomide doses equal to or greater than 125 mg/m2 (0.63 times the human dose of 200 mg/m2). These changes were most commonly seen at doses where mortalit…