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Temozolomide | CAS No: 85622-93-1 | GMP-certified suppliers
A medication that supports treatment of glioblastoma and anaplastic astrocytoma in adults, offering reliable central nervous system tumor management for oncology manufacturing needs.
Therapeutic categories
Alkylating ActivityAlkylating DrugsAntineoplastic AgentsAntineoplastic Agents, AlkylatingAntineoplastic and Immunomodulating AgentsBCRP/ABCG2 Substrates
Generic name
Temozolomide
Molecule type
small molecule
CAS number
85622-93-1
DrugBank ID
DB00853
Approval status
Approved drug, Investigational drug
ATC code
L01AX03
Primary indications
- Temozolomide is indicated in adult patients for the treatment of newly diagnosed glioblastoma concomitantly with radiotherapy and for use as maintenance treatment thereafter
- It is also indicated for the treatment of refractory anaplastic astrocytoma in adult patients or adjuvant therapy for adults with newly diagnosed anaplastic astrocytoma
Product Snapshot
- Temozolomide is an oral small-molecule API supplied mainly as capsules and as a parenteral lyophilized powder for solution
- It is used for glioblastoma and anaplastic astrocytoma in adult oncology settings
- It holds approved status in the US, EU, and Canada, with some presentations also listed as investigational
Clinical Overview
Temozolomide (CAS 85622-93-1) is an imidazotetrazine alkylating agent indicated for adult patients with newly diagnosed glioblastoma in combination with radiotherapy followed by maintenance therapy. It is also used in refractory anaplastic astrocytoma and as adjuvant treatment in newly diagnosed anaplastic astrocytoma. These tumours often exhibit compromised DNA repair capacity, contributing to initial responsiveness to alkylating chemotherapy.
Temozolomide is a small, lipophilic prodrug that is stable under acidic conditions and undergoes spontaneous nonenzymatic hydrolysis at physiological pH. This reaction forms MTIC, which decomposes to AIC and a methyl diazonium cation. The active cation methylates DNA at N7-guanine, N3-adenine, and O6-guanine. Persistent O6-methylguanine lesions trigger mismatch repair–mediated futile cycling and strand breaks, leading to apoptosis. Sensitivity is highest in tumours with reduced MGMT activity and intact mismatch repair, while MGMT overexpression or mismatch repair deficiency contributes to resistance.
Oral bioavailability is high, and the molecule crosses the blood–brain barrier, allowing therapeutic CNS exposure. Temozolomide is not enzyme dependent for activation and is cleared mainly by renal excretion of metabolites. The compound has a narrow therapeutic index.
Myelosuppression is the principal dose‑limiting toxicity and may be more pronounced in females and older adults. Requirements for baseline neutrophil and platelet counts and frequent hematologic monitoring are essential. Prophylaxis against Pneumocystis pneumonia is recommended during concomitant chemoradiation. Cases of myelodysplastic syndrome, secondary malignancies, and severe hepatotoxicity have been reported, warranting structured liver function monitoring. Embryo‑fetal toxicity has been demonstrated in animal studies, and contraception is required after treatment cessation.
Temozolomide is marketed under the trade name TEMODAR and is available in oral and intravenous formulations.
For API procurement, sourcing should prioritize manufacturers with robust controls for impurity profiles, stability of the imidazotetrazine structure, and validated handling conditions suitable for a cytotoxic alkylating agent with a narrow therapeutic index.
Temozolomide is a small, lipophilic prodrug that is stable under acidic conditions and undergoes spontaneous nonenzymatic hydrolysis at physiological pH. This reaction forms MTIC, which decomposes to AIC and a methyl diazonium cation. The active cation methylates DNA at N7-guanine, N3-adenine, and O6-guanine. Persistent O6-methylguanine lesions trigger mismatch repair–mediated futile cycling and strand breaks, leading to apoptosis. Sensitivity is highest in tumours with reduced MGMT activity and intact mismatch repair, while MGMT overexpression or mismatch repair deficiency contributes to resistance.
Oral bioavailability is high, and the molecule crosses the blood–brain barrier, allowing therapeutic CNS exposure. Temozolomide is not enzyme dependent for activation and is cleared mainly by renal excretion of metabolites. The compound has a narrow therapeutic index.
Myelosuppression is the principal dose‑limiting toxicity and may be more pronounced in females and older adults. Requirements for baseline neutrophil and platelet counts and frequent hematologic monitoring are essential. Prophylaxis against Pneumocystis pneumonia is recommended during concomitant chemoradiation. Cases of myelodysplastic syndrome, secondary malignancies, and severe hepatotoxicity have been reported, warranting structured liver function monitoring. Embryo‑fetal toxicity has been demonstrated in animal studies, and contraception is required after treatment cessation.
Temozolomide is marketed under the trade name TEMODAR and is available in oral and intravenous formulations.
For API procurement, sourcing should prioritize manufacturers with robust controls for impurity profiles, stability of the imidazotetrazine structure, and validated handling conditions suitable for a cytotoxic alkylating agent with a narrow therapeutic index.
Identification & chemistry
| Generic name | Temozolomide |
|---|---|
| Molecule type | Small molecule |
| CAS | 85622-93-1 |
| UNII | YF1K15M17Y |
| DrugBank ID | DB00853 |
Pharmacology
| Summary | Temozolomide is an imidazotetrazine prodrug that spontaneously converts to the reactive intermediate MTIC, generating a methyl diazonium species that methylates DNA. Its cytotoxic activity is driven primarily by O6‑guanine methylation, which triggers mismatch‑repair–dependent DNA strand breaks in tumors with low MGMT activity. The drug also produces systemic lymphodepletion, which can alter tumor‑associated immune populations and influence responses to immunotherapy. |
|---|---|
| Mechanism of action | Glioblastoma (glioblastoma multiforme) is the most common and aggressive adult primary brain tumour, accounting for 45.6% of all primary malignant brain tumours. Primarily defined histopathologically by necrosis and microvascular proliferation (WHO grade IV classification), glioblastomas are commonly treated through radiotherapy and concomitant alkylation-based chemotherapy with temozolomide.Temozolomide (TMZ) is a small (194 Da) lipophilic alkylating agent of the imidazotetrazine class that is stable at acidic pH, allowing for both oral and intravenous dosing, and can cross the blood-brain barrier to affect CNS tumours.After absorption, TMZ undergoes spontaneous nonenzymatic breakdown at physiological pH to form 5-(3-methyltriazen-1-yl) imidazole-4-carboxamide (MTIC), which then reacts with water to produce 5-aminoimidazole-4-carboxamide (AIC) and a highly reactive methyl diazonium cation.Brain tumours such as glioblastoma typically possess a more alkaline pH than healthy tissue, favouring TMZ activation within tumour tissue. The methyl diazonium cation is highly reactive and methylates DNA at the N7 position of guanine (N7-MeG, 70%), the N3 position of adenine (N3-MeA, 9%), and the O6 position of guanine (O6-MeG, 6%). Although more prevalent, N7-MeG and N3-MeA are rapidly repaired by the base excision repair pathway and are not primary mediators of temozolomide toxicity, although N3-MeA lesions are lethal if not repaired. By comparison, repair of O6-MeG requires action by the suicide enzyme methylguanine-DNA methyltransferase (MGMT), which removes the methyl group to restore guanine. If not repaired by MGMT, O6-MeG mispairs with thymine, activating the DNA mismatch repair (MMR) pathway that removes the thymine (not the O6-MeG), resulting in futile cycles of repair and eventual DNA strand breaks leading to apoptosis.As MMR activity is crucial for temozolomide cytotoxicity, cells that have reduced or absent MGMT function and an intact MMR pathway are the most sensitive to temozolomide treatment.Glioblastomas that upregulate MGMT downregulate MMR or alter both are resistant to TMZ, leading to treatment failure. More recently, increased interest has also been shown in the immunomodulatory effects of TMZ, related to its myelosuppressive effects. Counterintuitively, lymphodepletion may enhance the antitumour effects of cellular immunotherapy and improve the dynamics of memory cells by altering tumour-specific versus tumour-tolerant populations. The depletion of tumour-localized immunosuppressive T<sub>reg</sub> cells may contribute to an improved response to immunotherapy. Hence, TMZ treatment may also form the backbone of immunotherapy strategies against glioblastoma in the future. |
| Pharmacodynamics | Temozolomide is a prodrug of the imidazotetrazine class that requires nonenzymatic hydrolysis at physiological pH _in vivo_ to perform alkylation of adenine/guanine residues, leading to DNA damage through futile repair cycles and eventual cell death. Temozolomide treatment is associated with myelosuppression, which is likely to be more severe in females and geriatric patients. Patients must have an ANC of ≥1.5 x 10<sup>9</sup>/L and a platelet count of ≥100 x 10<sup>9</sup>/L before starting therapy and must be monitored weekly during the concomitant radiotherapy phase, on days one and 22 of maintenance cycles, and weekly at any point where the ANC/platelet count falls below the specified values until recovery. Cases of myelodysplastic syndrome and secondary malignancies, including myeloid leukemia, have been observed following temozolomide administration. Pneumocystis pneumonia may occur in patients undergoing treatment, and prophylaxis should be provided for patients in the concomitant phase of therapy with monitoring at all stages. Severe hepatotoxicity has also been reported, and liver testing should be performed at baseline, midway through the first cycle, before each subsequent cycle, and approximately two to four weeks after the last dose. Animal studies suggest that temozolomide has significant embryo-fetal toxicity; male and female patients should practice contraception up to three and six months following the last dose of temozolomide, respectively. |
Targets
| Target | Organism | Actions |
|---|---|---|
| DNA | Humans | cross-linking/alkylation |
ADME / PK
| Absorption | Temozolomide is rapidly and completely absorbed in the gastrointestinal tract and is stable at both acidic and neutral pH. Therefore, temozolomide may be administered both orally and intravenously with a median T<sub>max</sub> of one hour. Following a single oral dose of 150 mg/m<sup>2</sup>, temozolomide and its active MTIC metabolite had C<sub>max</sub> values of 7.5 μg/mL and 282 ng/mL and AUC values of 23.4 μg\*hr/mL and 864 ng\*hr/mL, respectively. Similarly, following a single 90-minute IV infusion of 150 mg/m<sup>2</sup>, temozolide and its active MTIC metabolite had C<sub>max</sub> values of 7.3 μg/mL and 276 ng/mL and AUC values of 24.6 μg\*hr/mL and 891 ng\*hr/mL, respectively. Temozolomide kinetics are linear over the range of 75-250 mg/m<sup>2</sup>/day. The median T<sub>max</sub> is 1 hour Oral temozolomide absorption is affected by food. Administration following a high-fat breakfast of 587 calories caused the mean C<sub>max</sub> and AUC to decrease by 32% and 9%, respectively, and the median T<sub>max</sub> to increase by 2-fold (from 1-2.25 hours). |
|---|---|
| Half-life | Temozolomide has a mean elimination half-life of 1.8 hours. |
| Protein binding | Temozolomide plasma protein binding varies from 8-36%, with an average of around 15%._In vitro_ binding experiments revealed approximate dissociation constants of 0.2-0.25 and 0.12 mM for temozolomide with human serum albumin (HSA) and alpha-1-acid glycoprotein (AGP), respectively; despite the slightly higher affinity for AGP, it is likely that temozolomide is predominantly bound to HSA due to its higher serum concentration. In addition, temozolomide binding to HSA results in delayed hydrolysis and a longer half-life than in buffer (1 versus 1.8 hours). |
| Metabolism | After absorption, temozolomide undergoes nonenzymatic chemical conversion to the active metabolite 5-(3-methyltriazen-1-yl) imidazole-4-carboxamide (MTIC) plus carbon dioxide and to a temozolomide acid metabolite, which occurs at physiological pH but is enhanced with increasing alkalinity.MTIC subsequently reacts with water to produce 5-aminoimidazole-4-carboxamide (AIC) and a highly reactive methyl diazonium cation, the active alkylating species.The cytochrome P450 system plays only a minor role in temozolomide metabolism. Relative to the AUC of temozolomide, the exposure to MTIC and AIC is 2.4% and 23%, respectively. |
| Route of elimination | Roughly 38% of administered temozolomide can be recovered over seven days, with 38% in the urine and only 0.8% in the feces. The recovered material comprises mainly metabolites: unidentified polar metabolites (17%), AIC (12%), and the temozolomide acid metabolite (2.3%). Only 6% of the recovered dose represents unchanged temozolomide. |
| Volume of distribution | Temozolomide has a mean apparent volume of distribution (%CV) of 0.4 (13%) L/kg. |
| Clearance | Temozolomide has a clearance of approximately 5.5 L/hr/m<sup>2</sup>. |
Formulation & handling
- Oral capsules show reduced absorption with food, so formulations are typically used in fasted conditions to limit variability and nausea.
- IV presentations rely on lyophilized powder requiring reconstitution under controlled conditions due to hydrolytic lability of the imidazotetrazine ring.
- As a small, highly soluble, low‑logP molecule, it is chemically unstable in aqueous solution, necessitating dry, protected storage and short post‑reconstitution hold times.
Regulatory status
| Lifecycle | Most core patent protections in the United States and Canada have lapsed, with final expiries occurring in 2023, indicating the API is now in a mature stage of its lifecycle. With established availability across Canada, the EU, and the US, the market environment is consistent with broadened generic participation. |
|---|
| Markets | Canada, EU, US |
|---|
Supply Chain
| Supply chain summary | Temozolomide supply is anchored by a small set of originator and early manufacturers, with Schering historically leading development and additional firms contributing to commercial production and packaging. Branded products have established distribution across the US, EU, and Canada. With key US and Canadian patents now expired, the product is already in a period of active or expanding generic competition. |
|---|
Safety
| Toxicity | The primary dose-limiting toxicity of temozolomide is myelosuppression, which can occur with any dose but is more severe at higher doses. Patients taking high doses experienced adverse reactions, including severe and prolonged myelosuppression, infections, and death. One patient who took 2000 mg/day for five days experienced pancytopenia, pyrexia, and multi-organ failure, which resulted in death. Patients experiencing an overdose should have complete blood counts monitored and provided with supportive care as necessary. |
|---|
High Level Warnings:
- Myelosuppression is the principal dose‑limiting toxicity
- Severe and prolonged cytopenias and secondary infections have been observed at elevated exposures
- Extreme overdose scenarios have produced pancytopenia, pyrexia, and multi‑organ failure, indicating the need for stringent exposure control and monitoring in manufacturing and handling environments
Temozolomide is a type of Alkylating agents
Alkylating agents are a vital subcategory of pharmaceutical active pharmaceutical ingredients (APIs) that play a significant role in cancer treatment. These compounds possess the ability to attach alkyl groups to the DNA molecule, effectively disrupting its structure and preventing cell replication. This mechanism of action makes alkylating agents potent chemotherapy drugs for various types of cancers.
Alkylating agents are often classified based on their chemical structure, which includes nitrogen mustards, ethylenimines, nitrosoureas, and alkyl sulfonates, among others. Each subclass exhibits unique chemical properties and therapeutic applications. For instance, nitrogen mustards like cyclophosphamide and mechlorethamine are used to treat lymphomas and leukemia, while nitrosoureas such as carmustine and lomustine are effective against brain tumors.
The alkylating agents' mode of action involves the transfer of alkyl groups to cellular components, primarily DNA. This leads to the formation of DNA adducts, cross-links, and DNA strand breaks, ultimately hindering DNA replication and causing cell death. The indiscriminate nature of alkylating agents can also affect healthy cells, leading to various side effects such as bone marrow suppression and gastrointestinal disturbances.
Despite their potential side effects, alkylating agents remain valuable tools in cancer therapy due to their broad spectrum of activity against different types of tumors. Ongoing research focuses on developing more selective and targeted alkylating agents to improve their therapeutic index and minimize adverse effects. The use of alkylating agents in combination with other chemotherapy drugs or radiation therapy is also being explored to enhance treatment outcomes and reduce drug resistance.
In conclusion, alkylating agents are an essential subclass of pharmaceutical APIs widely employed in cancer treatment. Their ability to disrupt DNA structure and impede cell replication makes them effective against various types of tumors, although careful management of side effects is necessary. Ongoing advancements and research continue to refine their therapeutic potential in the fight against cancer.
Temozolomide (Alkylating agents), classified under Anticancer drugs
Anticancer drugs belong to the pharmaceutical API (Active Pharmaceutical Ingredient) category designed specifically to combat cancer cells. These powerful medications play a crucial role in cancer treatment and are developed to target and destroy cancerous cells, preventing their growth and spread.
Anticancer drugs are classified based on their mode of action and can include various types such as chemotherapy drugs, targeted therapy drugs, immunotherapy drugs, and hormonal therapy drugs. Chemotherapy drugs work by interfering with the cell division process, thereby inhibiting the growth of cancer cells. Targeted therapy drugs, on the other hand, are designed to attack specific molecules or genes involved in cancer growth, minimizing damage to healthy cells. Immunotherapy drugs stimulate the body's immune system to recognize and destroy cancer cells. Hormonal therapy drugs are used in cancers that are hormone-dependent, such as breast or prostate cancer, to block the hormones that fuel cancer cell growth.
These APIs are typically synthesized through complex chemical processes in state-of-the-art manufacturing facilities. Stringent quality control measures ensure the purity, potency, and safety of these drugs. Anticancer APIs undergo rigorous testing and adhere to stringent regulatory guidelines before being approved for clinical use.
Due to their critical role in cancer treatment, anticancer drugs are in high demand worldwide. Researchers and pharmaceutical companies continually strive to develop new and more effective APIs in this category to enhance treatment outcomes and minimize side effects. The ongoing advancements in the field of anticancer drug development offer hope for improved cancer therapies and better patient outcomes.
Temozolomide API manufacturers & distributors
Compare qualified Temozolomide API suppliers worldwide. We currently have 18 companies offering Temozolomide API, with manufacturing taking place in 5 different countries. Use the table below to review supplier type, countries of origin, certifications, product portfolio and GMP audit availability.
| Supplier | Type | Country | Product origin | Certifications | Portfolio |
|---|---|---|---|---|---|
| Ampac Fine Chemicals | Producer | United States | United States | CoA, USDMF | 6 products |
| AXXO GmbH | Distributor | Germany | World | CoA, GMP, GDP, MSDS, USDMF | 243 products |
| Cipla | Producer | India | India | CoA, GMP, USDMF, WC | 164 products |
| Dalian Wista Pharma Co Lt... | Producer | China | China | CoA | 16 products |
| Formosa Labs | Producer | Taiwan | Taiwan | CEP, CoA, GMP, JDMF, USDMF | 36 products |
| Fujian South Pharma | Producer | China | China | CoA, WC | 7 products |
| Global Pharma Tek | Distributor | India | India | BSE/TSE, CoA, FDA, GMP, ISO9001, MSDS | 484 products |
| Hetero Drugs | Producer | India | India | CEP, CoA, GMP | 98 products |
| Hetero Labs | Producer | India | India | CoA, GMP, USDMF, WC | 90 products |
| Hubei Haosun Pharma | Producer | China | China | CoA, USDMF | 8 products |
| Ind-Swift Labs. | Producer | India | India | CoA, GMP, USDMF, WC | 27 products |
| Kromozome | Distributor | India | India | CoA, GMP | 17 products |
| Laurus Labs | Producer | India | India | CoA, GMP, WC | 50 products |
| Reliance Life Sciences | Producer | India | India | CoA, USDMF, WC | 11 products |
| Shilpa Medicare Ltd | Producer | India | India | BSE/TSE, CEP, CoA, EDMF/ASMF, GMP, ISO9001, MSDS, USDMF, WC | 54 products |
| Shivalik Rasayan Ltd. | Producer | India | India | CEP, CoA, GMP, USDMF, WC, WHO-GMP | 13 products |
| Sun Pharma | Producer | India | India | CoA, GMP, USDMF, WC | 219 products |
| Suzhou Lixin Pharmaceutic... | Producer | China | China | BSE/TSE, CEP, CoA, EDMF/ASMF, GMP, MSDS | 34 products |
When sending a request, specify which Temozolomide API quality you need: for example EP (Ph. Eur.), USP, JP, BP, or another pharmacopoeial standard, as well as the required grade (base, salt, micronised, specific purity, etc.).
Use the list above to find high-quality Temozolomide API suppliers. For example, you can select GMP, FDA or ISO certified suppliers. Visit our help page to learn more about sourcing APIs via Pharmaoffer.
Frequently asked questions about Temozolomide API
Sourcing
What matters most when sourcing GMP-grade Temozolomide?
Key considerations include verifying GMP compliance for the US, EU, and Canada and ensuring the manufacturer has an established regulatory track record. Given the limited pool of originator and early manufacturers, supply reliability and continuity are important. It is also useful to confirm that the supplier’s material aligns with current generic competition dynamics following US and Canadian patent expiry.
Which documents are typically required when sourcing Temozolomide API?
Request the core API documentation set: CoA (17 companies), GMP (12 companies), USDMF (11 companies), WC (9 companies), CEP (5 companies). Confirm versions and validity dates match the destination market to avoid delays in qualification.
Which manufacturers are known to produce Temozolomide API?
Known or reported manufacturers for Temozolomide: Suzhou Lixin Pharmaceutical CO.,LTD., Global Pharma Tek, Shivalik Rasayan Ltd., Shilpa Medicare Ltd, AXXO GmbH. Evaluate their GMP history, scale, and regional coverage before requesting dossiers or allocating demand.
How can I request quotes for Temozolomide API from GMP suppliers?
Submit quote requests through the supplier listings with your specs and required documents (specifications, target volume, delivery timeline, and destination). Providing consistent details upfront speeds comparable offers and clarifies technical feasibility.
Is a GMP audit report available for Temozolomide manufacturers?
Audit reports may be requested for Temozolomide: 6 GMP audit reports available. Confirm the scope and recency of any audit before relying on it for qualification decisions.
How many suppliers offer Temozolomide API on Pharmaoffer?
Reported supplier count for Temozolomide: 17 verified suppliers. Filter listings by certifications, regions, and delivery options to match your qualification plan.
Which countries are known to manufacture Temozolomide API?
Production countries reported for Temozolomide: India (10 producers), China (4 producers), Taiwan (1 producer). Knowing the manufacturing geography helps anticipate logistics lead times and import compliance needs.
Which certifications do suppliers of Temozolomide usually hold?
Common certifications for Temozolomide suppliers: CoA (17 companies), GMP (12 companies), USDMF (11 companies), WC (9 companies), CEP (5 companies). Always verify issuing authorities and expiry dates when reviewing audit packages.
Technical
What is Temozolomide (CAS 85622-93-1) used for?
Temozolomide is used to treat malignant brain tumours, primarily newly diagnosed glioblastoma in combination with radiotherapy followed by maintenance therapy. It is also used for refractory anaplastic astrocytoma and as adjuvant therapy in newly diagnosed anaplastic astrocytoma. Its activity comes from DNA methylation after conversion to the active compound MTIC, which is particularly effective in tumours with reduced MGMT repair activity.
Which therapeutic class does Temozolomide fall into?
Temozolomide belongs to the following therapeutic categories: Alkylating Activity, Alkylating Drugs, Antineoplastic Agents, Antineoplastic Agents, Alkylating, Antineoplastic and Immunomodulating Agents. This positioning helps teams compare alternative APIs, anticipate pharmacology expectations, and align early research priorities.
What conditions is Temozolomide mainly prescribed for?
The primary indications for Temozolomide: Temozolomide is indicated in adult patients for the treatment of newly diagnosed glioblastoma concomitantly with radiotherapy and for use as maintenance treatment thereafter, It is also indicated for the treatment of refractory anaplastic astrocytoma in adult patients or adjuvant therapy for adults with newly diagnosed anaplastic astrocytoma. These use cases frame the target patient populations and help prioritize formulation and safety evaluations.
How does Temozolomide work?
Glioblastoma (glioblastoma multiforme) is the most common and aggressive adult primary brain tumour, accounting for 45.6% of all primary malignant brain tumours. Primarily defined histopathologically by necrosis and microvascular proliferation (WHO grade IV classification), glioblastomas are commonly treated through radiotherapy and concomitant alkylation-based chemotherapy with Temozolomide.Temozolomide (TMZ) is a small (194 Da) lipophilic alkylating agent of the imidazotetrazine class that is stable at acidic pH, allowing for both oral and intravenous dosing, and can cross the blood-brain barrier to affect CNS tumours.After absorption, TMZ undergoes spontaneous nonenzymatic breakdown at physiological pH to form 5-(3-methyltriazen-1-yl) imidazole-4-carboxamide (MTIC), which then reacts with water to produce 5-aminoimidazole-4-carboxamide (AIC) and a highly reactive methyl diazonium cation.Brain tumours such as glioblastoma typically possess a more alkaline pH than healthy tissue, favouring TMZ activation within tumour tissue.
The methyl diazonium cation is highly reactive and methylates DNA at the N7 position of guanine (N7-MeG, 70%), the N3 position of adenine (N3-MeA, 9%), and the O6 position of guanine (O6-MeG, 6%). Although more prevalent, N7-MeG and N3-MeA are rapidly repaired by the base excision repair pathway and are not primary mediators of Temozolomide toxicity, although N3-MeA lesions are lethal if not repaired. By comparison, repair of O6-MeG requires action by the suicide enzyme methylguanine-DNA methyltransferase (MGMT), which removes the methyl group to restore guanine. If not repaired by MGMT, O6-MeG mispairs with thymine, activating the DNA mismatch repair (MMR) pathway that removes the thymine (not the O6-MeG), resulting in futile cycles of repair and eventual DNA strand breaks leading to apoptosis.As MMR activity is crucial for Temozolomide cytotoxicity, cells that have reduced or absent MGMT function and an intact MMR pathway are the most sensitive to Temozolomide treatment.Glioblastomas that upregulate MGMT downregulate MMR or alter both are resistant to TMZ, leading to treatment failure.
More recently, increased interest has also been shown in the immunomodulatory effects of TMZ, related to its myelosuppressive effects. Counterintuitively, lymphodepletion may enhance the antitumour effects of cellular immunotherapy and improve the dynamics of memory cells by altering tumour-specific versus tumour-tolerant populations. The depletion of tumour-localized immunosuppressive Treg cells may contribute to an improved response to immunotherapy. Hence, TMZ treatment may also form the backbone of immunotherapy strategies against glioblastoma in the future.
What should someone know about the safety or toxicity profile of Temozolomide?
Temozolomide’s safety profile is dominated by dose‑dependent myelosuppression, with risks of severe neutropenia, thrombocytopenia, and secondary infections, particularly at higher exposures. Overdose scenarios have caused pancytopenia, pyrexia, and multi‑organ failure, underscoring the need for strict handling and exposure controls. Hepatotoxicity, Pneumocystis pneumonia during chemoradiation, and rare cases of myelodysplastic syndrome or secondary malignancies have been reported, requiring structured laboratory monitoring. Embryo‑fetal toxicity has been demonstrated, and effective contraception is required after treatment.
What are important formulation and handling considerations for Temozolomide as an API?
Temozolomide is hydrolytically unstable in aqueous environments, so it is handled and stored in a dry state with protection from moisture, and reconstituted IV products require controlled preparation and short hold times. The oral API is typically formulated to be taken under fasted conditions because food reduces absorption and increases variability. Its small, highly soluble nature and chemical lability limit opportunities for aqueous formulations, making solid or lyophilized forms preferable. Care is taken to avoid alkaline conditions, which accelerate conversion to metabolites.
Is Temozolomide a small molecule?
Temozolomide is classified as a small molecule. That classification shapes process design, impurity profiling, and analytical control strategies.
Are there special stability concerns for oral Temozolomide?
Yes. Oral Temozolomide is chemically unstable in aqueous environments, so the capsules require dry, protected storage. Although stable at acidic and neutral pH in the GI tract, its absorption decreases when taken with food, creating variability in exposure. For this reason, administration under fasted conditions is recommended to limit variability.
Regulatory
Where is Temozolomide approved or in use globally?
Temozolomide is reported as approved in the following major regions: Canada, EU, US. Understanding geographic coverage informs regulatory filings, supply planning, and risk assessments before escalating procurement.
What’s the regulatory and patent landscape for Temozolomide right now?
Temozolomide is authorized for use in Canada, the EU, and the US, where it is regulated as an established oncology active ingredient. Patent status varies by jurisdiction and product formulation, with protections typically expiring on different timelines depending on regional patent law.
Pharmaoffer
How does Pharmaoffer’s Smart Sourcing Service help with Temozolomide procurement?
Pharmaoffer's Smart Sourcing Service coordinates compliant suppliers, documentation, and competitive quotes for Temozolomide. It centralizes outreach, follow-ups, and document validation to shorten procurement timelines.
Is Temozolomide included in the PRO Data Insights coverage?
PRO Data Insights coverage for Temozolomide: 526 verified transactions across 199 suppliers and 115 buyers worldwide. Use the dataset to benchmark suppliers and monitor regulatory activity where available.
Where can I access the API market report for Temozolomide?
Market report availability for Temozolomide: Report Available. The report highlights demand trends, pricing drivers, and supplier landscape insights for procurement planning.
