Temodar

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Temodar

Medically reviewed

Rosario Oropesa

Last updated on 22/12/2025

This page provides general, reference-level information compiled from official medical sources. It is not a substitute for professional medical advice, diagnosis, or treatment. For decisions about your health, please consult a qualified healthcare professional.

Overview of Temodar

Quick Facts

Property Description
Active ingredient Temozolomide (TMZ)
Form Capsule (oral), Powder for Injection (intravenous)
Pharmacological class Alkylating Agent, Antineoplastic Agent
Common purpose To slow or stop the growth of malignant cells
Origin Synthetic compound, Imidazotetrazine derivative

Core Identity and Classification

Temodar is a prescription-only chemotherapy drug used in the clinical management of conditions characterized by abnormal cellular proliferation. Its active ingredient is Temozolomide (TMZ), a synthetic compound that is officially classified as an antineoplastic agent.

Temozolomide is formally categorized as an alkylating agent and is an Imidazotetrazine derivative. This classification is clinically recognized for its established role in certain therapeutic protocols, supported by numerous pharmacological studies. The medicine is manufactured as a single-ingredient product, available for different routes of administration: as an oral capsule and as a lyophilized powder used to prepare an intravenous solution.


High-Level Action and Purpose

Temozolomide functions as a prodrug, a type of compound that is largely inactive upon administration but is specifically designed to undergo a rapid, non-enzymatic chemical transformation within the body to form its potent, active cytotoxic agent. This unique chemical property aids the medicine in reaching target areas, such as the central nervous system.

The activated form works by delivering a methyl group to the genetic material (DNA) of rapidly dividing cells, a process called alkylation. This chemical alteration damages the DNA, preventing the cells from replicating and triggering their eventual self-destruction (apoptosis). This action serves the general purpose of helping to limit the advancement of the underlying condition by reducing the malignant cell population.

What side effects are possible with Temodar?

The safety profile of Temodar (temozolomide) is officially documented by regulatory authorities, with adverse reactions categorized by their frequency and effect on specific body systems.

Adverse Reaction Scope

Classification Organ System Affected Examples
Very Common (≥10%) Blood and Lymphatic, Nervous, Gastrointestinal Thrombocytopenia, Lymphopenia, Nausea, Vomiting, Headache, Fatigue, Alopecia
Common (≥1% to <10%) Gastrointestinal, Infections, Skin Diarrhea, Anemia, Leukopenia, Rash, Opportunistic Infections

Myelosuppression, which is the suppression of bone marrow activity, is the primary concern, leading to a reduction in blood cell counts (lymphopenia, neutropenia, and thrombocytopenia). The lowest blood cell counts, or nadir, typically occur between Day 21 and Day 28 of a treatment cycle.

Serious Safety Considerations

The official labeling notes the risk of serious adverse reactions, including potentially fatal events. These include severe myelosuppression and fatal hepatic toxicity (liver failure). The risk of opportunistic infections, such as Pneumocystis jirovecii Pneumonia (PJP), is also officially documented, particularly when the medicine is used concurrently with radiotherapy.

Population-Specific Safety: Older adults (70 years of age and older) and women appear to be at an increased risk of developing neutropenia and thrombocytopenia. Caution is advised for individuals with severe hepatic or renal impairment, as comprehensive safety data is limited in these groups. The medicine is formally contraindicated in individuals with a known hypersensitivity to the active substance or to Dacarbazine.

This structure of official safety information primarily frames the risks around hematological toxicity, providing a clear regulatory basis for monitoring blood counts throughout the course of treatment.

Overdose and Emergency Response

Overdose and when to seek help

Overdose with Temodar is characterized by an exaggeration of its established dose-limiting effect, which is severe myelosuppression. This condition affects the hematopoietic system and can lead to dangerously low blood cell counts. Officially documented laboratory manifestations of severe exposure include an Absolute Neutrophil Count (ANC) less than 0.5 imes 10^9/ L or a Platelet Count less than 10 imes 10^9/ L. Acute gastrointestinal symptoms such as severe nausea, vomiting, and diarrhea may also be present.

These severe hematological abnormalities define life-threatening clinical outcomes, including the risk of fatal infectious or hemorrhagic complications. Official regulatory documents also note that severe and sometimes fatal hepatotoxicity has been reported following treatment.

If an overdose is suspected, seek immediate medical attention or contact emergency medical services immediately. The official prescribing information states that no specific antidote is known for Temozolomide exposure. Overdose management is therefore limited to supportive measures to manage the resulting toxicities. As a mandatory requirement, Complete Blood Count (CBC) monitoring must be performed weekly until blood cell counts return to acceptable levels. Specific considerations exist for geriatric patients (ge 70 years), who are documented to be at an increased risk of severe myelosuppression.

Therapeutic Uses of Temodar

What Temodar Treats: Main Uses and Benefits

Temodar is commonly used in the neuro-oncology domain to manage certain primary central nervous system cancers, such as Glioblastoma Multiforme (GBM) and Anaplastic Astrocytoma (AA). Its therapeutic scope includes adult patients with newly diagnosed GBM, and it is also relevant for adults and children in certain age groups with malignant glioma, such as recurrent AA.

This medication is generally considered relevant in conditions presenting with systemic or localized discomfort and is applied in clinical settings that involve acute or unstable symptom patterns. The primary indications are GBM and AA, and its use is considered relevant in managing both newly diagnosed disease, often concurrently with radiation, and recurrent/refractory disease.

By acting on the malignant cells, Temodar generally supports the management of neurological symptom clusters associated with the tumor mass. Controlling malignant progression may assist with easing symptoms related to physical discomfort, such as headache, nausea, vomiting, and focal neurological deficits. This functional support generally assists with maintaining functional stability and helps improve day-to-day comfort during symptomatic periods.


Quick Fact: Supportive Management of Tumor-Related Discomfort

Symptom Type Therapeutic Benefit
Physical Discomfort Supports easing symptoms related to mass effect (e.g., headache).
Functional Strain Assists with supporting functional stability (e.g., addressing factors that may contribute to worsening focal deficits).
Clinical Context Relevant for conditions characterized by periods of heightened symptoms (e.g., recurrent high-grade glioma).

Regulatory References

  1. European Medicines Agency overview of Temodal (temozolomide)

Eligibility and Restrictions for Use

Who Can and Cannot Use Temodar?

The official regulatory guidelines strictly define the patient populations eligible for Temodar (temozolomide) treatment based on age, existing conditions, and physiological status.

Category Regulatory Status and Limitations
Approved Age Groups Adults and pediatric patients ge 3 years of age for specified malignant glioma indications.
Use Not Established Safety and efficacy have not been established in children under the age of 3 years; no data are available for this group.
Conditional Eligibility Treatment is withheld unless the Absolute Neutrophil Count (ANC) is mathbfge 1.5 imes 10^9/L and Platelet Count is mathbfge 100 imes 10^9/L.
Contraindicated Patients with known hypersensitivity to temozolomide or the related drug dacarbazine (DTIC), or those with severe myelosuppression.
Pregnancy/Lactation Should not be administered during pregnancy due to potential fetal harm. Breast-feeding should be discontinued.
Organ Impairment Caution should be exercised when administered to patients with severe renal impairment or severe hepatic impairment, as data is limited.

Regulatory documentation defines eligibility by setting absolute exclusions based on hypersensitivity and severe myelosuppression. The official label also places strict age-based limitations by excluding children under 3 and mandates caution for patients with severe organ impairment due to a lack of complete data in those populations.

What should I know about interactions with other medicines?

Interactions with other medicines and products

Official regulatory information for Temodar (Temozolomide) documents specific interaction patterns that affect drug exposure, mandate timing requirements, and include formal substance-based prohibitions. This information is derived exclusively from regulatory documents such as the FDA Prescribing Information and the European Medicines Agency (EMA) SmPC.


Documented Pharmacokinetic and Substance Interactions

Category Interacting Entity Official Regulatory Statement
Exposure-Altering Valproic acid Co-administration decreases the oral clearance of Temozolomide.
Contraindication Dacarbazine (DTIC) Use is contraindicated in patients with known hypersensitivity to Dacarbazine, a chemically related compound.

Administration Timing and Population Constraints

Category Constraint or Condition Official Regulatory Statement
Timing Rule Food Administration requires the fasting state (without food) as specified in European prescribing information.
Population Caution Severe Hepatic Impairment Caution is advised due to a lack of complete pharmacokinetic data in this specific population.
Population Caution Severe Renal Impairment Caution is advised due to a lack of complete pharmacokinetic data in this specific population.

These constraints define the official drug-drug and drug-substance profile, focusing strictly on required timing rules and documented changes to systemic exposure.

Mechanism of Action

Non-Enzymatic Activation and DNA Alkylation

Temozolomide operates as a prodrug, undergoing rapid, non-enzymatic chemical hydrolysis to form the cytotoxic agent, the methyldiazonium cation. This active species exerts its primary effect by chemically attaching a methyl group to the cell's genetic material (DNA), a process known as alkylation. The primary cytotoxic alkylation occurs at the O^6 position of the guanine base ( O^6 -MeG), which initiates the subsequent cascade.

Overloading the DNA Mismatch Repair (MMR) Pathway

The O^6 -MeG lesion triggers the DNA Mismatch Repair (MMR) system, which attempts to fix the resulting DNA mispairing. This leads to repeated, failed repair cycles known as futile cycling. This sustained activity of the cellular repair pathway generates substantial secondary damage in the form of DNA strand breaks.

Induction of Apoptosis and MGMT Resistance

The accumulation of DNA strand breaks triggers the cell's G2/M cell cycle arrest and subsequently activates the intrinsic apoptosis pathway (programmed cell death). This physiological outcome leads to the controlled elimination of the target cell population. This mechanism is significantly constrained by the activity of the MGMT enzyme, which can directly and enzymatically remove the cytotoxic O^6 -MeG lesion, functionally bypassing the drug's intended action and preventing the induction of apoptosis.

Dosage and Administration Information

Official Administration Guidelines

Temodar (temozolomide) is administered either orally via capsules or intravenously (IV) as an infusion, with the dose for both forms being identical and calculated based on the patient's Body Surface Area (m^2). The medication follows a highly standardized, cyclic protocol.

Dosing Schedule and Frequency

Treatment Phase Daily Dose Range Schedule Duration
Newly Diagnosed GBM - Concomitant 75 mg/m^2/ day Once daily 42 days (up to 49 days) with radiotherapy
Maintenance/Monotherapy 150 mg/m^2/ day to 200 mg/m^2/ day Once daily for 5 consecutive days Up to 6 cycles (28 days per cycle)

For maintenance and monotherapy, Temodar is taken for 5 days, followed by a 23-day treatment break, completing one 28-day cycle. Dose adjustments (reduction or holding) are mandatory and are governed by specific hematological toxicity thresholds (Absolute Neutrophil Count and Platelet Count) observed in the previous cycle.

Practical Administration Instructions

Oral Use: Capsules must be swallowed whole with water and must not be opened, chewed, or crushed. They should be taken on an empty stomach—such as at bedtime or at least one hour before a meal—and consistently at the same time each day. If vomiting occurs immediately after administration, a second dose should not be taken that day. If a dose is missed, it should be taken as soon as possible, unless the next scheduled dose is due within 12 hours.

Intravenous (IV) Use: The IV formulation is administered as a diluted infusion over a 90-minute period. While dose adjustments are not explicitly required for older adults or in cases of severe renal/hepatic impairment, caution is advised in these specific populations.

Recent Clinical Evidence

Research Evidence / Overview of Studies for Temodar

This section provides an overview of the official research evidence for Temodar (temozolomide), summarizing the types of studies that have been conducted and the findings reported by authoritative governmental and intergovernmental sources. The findings describe group patterns and research context, not individual predictions or clinical recommendations.


Evidence for Newly Diagnosed Glioblastoma Multiforme (GBM)

The primary body of evidence for the clinical evaluation of Temodar in newly diagnosed Glioblastoma Multiforme (GBM) comes from large-scale, international Randomized Controlled Trials (RCTs). These studies were designed to evaluate the outcomes of patients who received Temodar alongside radiation therapy compared to those who received radiation therapy alone. Researchers specifically examined critical endpoints like Overall Survival (OS) and Progression-Free Survival (PFS).

Studies monitored outcomes in the combination group, and findings describe patterns where survival measurements were longer compared to the radiation-alone group. Research also explored the Health-Related Quality of Life (HRQoL); studies report how symptoms evolved in the observed populations, with measured scores tracked across both comparison groups.

Molecular Markers and Study Subgroups

Clinical research for newly diagnosed GBM was studied for how outcomes were affected by the tumor's genetic features, such as the MGMT promoter methylation status. The data show patterns related to this molecular status: favorable outcomes related to survival were more often monitored in patients whose tumors exhibited the methylated MGMT status. This evidence contributes to understanding symptom patterns in observed populations.


Evidence for Recurrent and Refractory Anaplastic Astrocytoma (AA)

The initial evidence supporting the clinical evaluation of Temodar for Anaplastic Astrocytoma (AA) that has returned or progressed was derived mainly from Single-arm, Multicenter Phase II Clinical Trials. These non-comparative trials examined anti-tumor activity by tracking endpoints such as the Objective Response Rate (ORR) and the rate of Progression-Free Survival at 6 months (PFS6). Findings describe patterns observed in these studies, reporting objective response measurements and the length of time patients remained without documented disease progression.


Research Gaps and What Remains Uncertain

The evidence base, while derived from high-quality studies for some uses, still contains areas where certainty remains low. A major research focus is the persistent issue of intrinsic or acquired resistance to the compound; findings indicate that resistance mechanisms was studied for its association with the outcomes observed in the studied populations. Furthermore, dedicated comparative evidence for the indication of recurrent/refractory AA is lacking, as initial approval was based on single-arm studies.

Frequently Asked Questions (FAQ)

Common questions about Temodar (FAQ)


Q: Can Temodar interact with common over-the-counter pain relievers or supplements?

A: Official studies listed in regulatory documents mainly focus on how the medicine interacts with certain supportive drugs, such as corticosteroids or anti-nausea medications, and they note no significant influence on Temodar's clearance. The regulatory label does not broadly address interactions with common over-the-counter pain relievers or general nutritional supplements.


Q: How long after stopping Temodar is it necessary to continue using birth control?

A: Official guidance indicates that females of reproductive potential use effective contraception throughout treatment and for at least 6 months after the last dose. Males who have partners who are pregnant or who could become pregnant use effective barrier contraception during treatment and for at least 3 months after the final dose.


Q: What information is available about Temodar use during pregnancy or breastfeeding?

A: Regulatory documents state that the medicine can cause fetal harm, and women of reproductive potential are advised of this potential risk. Official documentation advises that breast-feeding be discontinued during treatment because it is not known if the medicine is excreted into human milk.


Q: Are there certain age groups that experience more side effects from Temodar?

A: Official labeling indicates that older adults (specifically those 70 years of age and older) and women have been found to have a higher reported incidence of severe low blood cell counts (Grade 4 neutropenia and thrombocytopenia) during the initial treatment cycle compared to other patient groups.


Q: What is the difference between Temodar and other similar chemotherapy medicines?

A: The medicine is chemically classified as a single-ingredient alkylating agent of the imidazotetrazine class. It is described as a prodrug, which means it is an inactive substance that becomes chemically active only after it is metabolized within the body. This classification defines how it differs from other chemotherapy agents.


Q: Can Temodar be used for brain tumors other than glioblastoma and astrocytoma?

A: According to the FDA and other official bodies, the medicine is specifically indicated for adult patients with newly diagnosed glioblastoma multiforme and for adult patients with refractory anaplastic astrocytoma (an astrocytoma that has returned or progressed).


Q: Is it normal to feel very tired or fatigued while on Temodar treatment?

A: Clinical trial data included in regulatory documents classify fatigue as a very common adverse reaction. This means it has been reported to occur in 10% or more of patients receiving the medicine.


Q: Is hair loss from Temodar treatment temporary or permanent?

A: Alopecia (hair loss) is listed as a very common adverse reaction. Patient information derived from clinical reports often describes this side effect as generally temporary and reversible once treatment is finished, although permanent hair loss has been reported in certain cases.


Q: Can Temodar cause changes in my taste or sense of smell?

A: Clinical trial data included in official documents list taste perversion (changes in the sense of taste) as a reported adverse reaction. Changes to the sense of smell are not explicitly listed in the core documents.


Q: What are the signs of a serious infection that should be watched for during Temodar treatment?

A: Official guidance indicates that due to the risk of infection from low blood counts, signs such as an unexplained fever, chills, cough, or sore throat should be recognized as potential symptoms.


Q: Can Temodar cause problems with memory or concentration?

A: Official regulatory-derived patient guidance documents list adverse reactions related to the nervous system, such as amnesia (memory loss) and confusion. These are conditions that may affect memory or concentration.


Q: What is the risk of developing a secondary cancer years after taking Temodar?

A: The official labeling includes a formal warning that the incidence of secondary malignancies (new cancers) is increased. Cases of myelodysplastic syndrome and secondary malignancies, including myeloid leukemia, have been observed in patients following the administration of the medicine.


Q: How long does Temodar stay in the body after the last dose?

A: According to the pharmacokinetics section in regulatory documents, the medicine has a mean terminal plasma half-life ( t1/2) of approximately 1.8 hours. The half-life is the time it takes for the concentration of the medicine in the blood to decrease by half.


Q: Is it safe to get vaccines while I am undergoing treatment with Temodar?

A: Because the medicine has immunosuppressive properties, official guidance indicates that the administration of live-attenuated vaccines is generally not recommended during treatment. This is due to the potential for a diminished immune response or an increased risk of infection.


Q: What should I do if a Temodar capsule accidentally breaks or the powder is visible?

A: Regulatory documents advise taking rigorous precautions to avoid inhalation or contact with the skin or mucous membranes if a capsule is opened or damaged. Official guidance indicates that if contact with the skin occurs, the area should be washed with soap and water.


Q: What is the reason Temodar is sometimes taken together with radiation therapy?

A: The use of the medicine alongside radiation therapy is based on research studies. These studies suggest that the combined approach may be more effective in controlling the malignant cell population than when radiation therapy is used alone.


Q: Is there a different way to take Temodar if I have trouble swallowing the capsules?

A: The medicine is available in both an oral capsule formulation and as an intravenous (IV) infusion formulation. The IV infusion formulation may be an option if swallowing the capsules presents difficulty.


Q: Why is there a concern about using live vaccines while on Temodar?

A: The concern relates to the medicine's potential for immunosuppressive effects due to its action on the immune system. This can lead to a diminished therapeutic response to the vaccine or an increased risk of infection.


Q: Is it possible for Temodar to cause changes in mood or anxiety?

A: Adverse reactions listed in regulatory-derived patient guidance documents include psychiatric conditions such as anxiety and mental depression.


Q: Does Temodar cause a skin rash, and when should I be concerned about it?

A: Rash is listed as a common adverse reaction. Official postmarketing experience has reported severe reactions, including Toxic Epidermal Necrolysis and Stevens-Johnson syndrome, which are officially documented as serious adverse reactions that require prompt medical awareness.


Q: Does Temodar have any reported effects on hearing or vision?

A: Clinical trial data included in regulatory documents list blurred vision as a reported adverse reaction. Official documents do not commonly list effects on hearing.


Q: How should unused or expired Temodar capsules be safely disposed of?

A: As the medicine is classified as a hazardous drug, unused or expired capsules must be disposed of according to special handling procedures for cytotoxic drugs. The medication must not be flushed down the toilet or drain.


Q: Does Temodar have a known effect on weight (loss or gain)?

A: Official adverse reaction profiles list anorexia (loss of appetite) as a common effect. Unusual weight gain is also reported in patient guidance derived from clinical data.


Q: What is the potential impact of Temodar on a patient's sex life?

A: Regulatory documents indicate that the medicine is documented to potentially affect fertility in males and may impair the ability to father a child.


Q: Can taking Temodar cause sleep problems or insomnia?

A: Insomnia (trouble sleeping) is listed as a reported adverse reaction in regulatory-derived patient guidance documents.


Q: What are the long-term effects of Temodar treatment that patients should be aware of?

A: One formally documented long-term effect reported in regulatory documents is the increased risk of secondary malignancies (new cancers), including myelodysplastic syndrome and myeloid leukemia, which can occur following treatment.


Q: Does Temodar interact with common anti-nausea medications?

A: Drug interaction studies mentioned in the regulatory label show that co-administration of common anti-nausea agents, such as ondansetron or prochlorperazine, did not influence the clearance of the medicine in the body.


Q: What are the requirements for caregivers when handling Temodar capsules?

A: As a cytotoxic (hazardous) drug, official regulatory documentation indicates that caregivers take precautions, including following special handling and disposal procedures and avoiding inhalation or contact with the skin or mucous membranes if a capsule is broken.

How should Temodar be stored and disposed of?

The official storage and disposal guidelines for Temodar are dictated by regulatory classifications that designate it as a hazardous drug, requiring specific handling and temperature controls.


Official Storage Requirements

Formulation Required Temperature Stability/Constraint
Capsules Controlled Room Temperature (68-77 F) Must be protected from excess moisture and heat.
Injection Vials (Intact) Refrigerated (36-46 F) Must reach room temperature before reconstitution.

Handling and Disposal Rules

Temodar must be kept in the tightly closed container it was dispensed in, and the capsules or vials should not be opened or damaged to prevent exposure to the cytotoxic powder. The medication must be kept out of the sight and reach of children in a secure location.

As a hazardous drug, Temodar requires following special handling and disposal procedures for anticancer drugs. Unused or expired medication must not be flushed down the toilet or drain.

Attention! Always consult to a doctor or pharmacist before using pills or medicines.

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