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Etoposide | CAS No: 33419-42-0 | GMP-certified suppliers
A medication that treats refractory testicular tumors, small cell lung cancer, lymphomas, leukemias, and glioblastoma through combination chemotherapy with antineoplastic benefits.
Therapeutic categories
Primary indications
- For use in combination with other chemotherapeutic agents in the treatment of refractory testicular tumors and as first line treatment in patients with small cell lung cancer
- Also used to treat other malignancies such as lymphoma, non-lymphocytic leukemia, and glioblastoma multiforme
Product Snapshot
- Etoposide is available as an oral capsule and various injectable solutions including lyophilized powders for parenteral administration
- It is primarily indicated for use in combination chemotherapy regimens targeting refractory testicular tumors, small cell lung cancer, lymphoma, non-lymphocytic leukemia, and glioblastoma multiforme
- This API holds regulatory approval in key markets including the United States and Canada
Clinical Overview
Clinically, etoposide is indicated for use in refractory testicular tumors and as a first-line treatment in small cell lung cancer. Additional oncological applications include treatment of lymphoma, non-lymphocytic leukemia, and glioblastoma multiforme.
The pharmacological activity of etoposide arises from its inhibition of DNA topoisomerase II, an enzyme critical for relieving torsional strain during DNA replication and transcription. Etoposide stabilizes the transient DNA-topoisomerase II complex, preventing re-ligation of double-stranded DNA breaks. This results in the accumulation of DNA strand breaks, predominantly during the S and G2 phases of the cell cycle, leading to cell cycle arrest and apoptosis. The anti-tumor efficacy is associated with inhibition of topoisomerase II alpha isoform; inhibition of the beta isoform is linked with carcinogenic risk, not therapeutic effect.
Pharmacodynamically, etoposide exhibits dose-dependent effects: at concentrations above 10 µg/mL, mitotic cell lysis occurs, whereas lower concentrations (0.3 to 10 µg/mL) inhibit progression into prophase. The drug does not interfere with microtubule assembly.
Key ADME characteristics include metabolism primarily via cytochrome P450 enzymes CYP3A4, CYP1A2, and CYP2E1, and conjugation by UGT1A1. Etoposide is a substrate and inhibitor of P-glycoprotein and displays a narrow therapeutic index.
Safety considerations emphasize etoposide’s myelosuppressive and cardiotoxic potential, necessitating careful monitoring during treatment. It is classified among enzyme inhibitors with a notable toxicity profile, and its carcinogenic potential underscores the need for controlled clinical usage.
For sourcing, the etoposide API requires high purity with strict adherence to pharmacopeial standards reflecting its narrow therapeutic range and complex metabolism. Manufacturers must ensure consistent quality and impurity profiles to minimize variability and support regulatory compliance in global pharmaceutical markets.
Identification & chemistry
| Generic name | Etoposide |
|---|---|
| Molecule type | Small molecule |
| CAS | 33419-42-0 |
| UNII | 6PLQ3CP4P3 |
| DrugBank ID | DB00773 |
Pharmacology
| Summary | Etoposide is an antineoplastic agent that selectively inhibits DNA topoisomerase II alpha, disrupting DNA re-ligation during the S and G2 phases of the cell cycle. This inhibition leads to DNA strand breaks and errors in DNA synthesis, resulting in apoptosis of cancer cells. Its activity is dose-dependent, with distinct effects on cell cycle progression and mitotic cell lysis. |
|---|---|
| Mechanism of action | Etoposide inhibits DNA topoisomerase II, thereby inhibiting DNA re-ligation. This causes critical errors in DNA synthesis at the premitotic stage of cell division and can lead to apoptosis of the cancer cell. Etoposide is cell cycle dependent and phase specific, affecting mainly the S and G2 phases of cell division. Inhibition of the topoisomerase II alpha isoform results in the anti-tumour activity of etoposide. The drug is also capable of inhibiting the beta isoform but inhibition of this target is not associated with the anti-tumour activity. It is instead associated with the carcinogenic effect. |
| Pharmacodynamics | Etoposide is an antineoplastic agent and an epipodophyllotoxin (a semisynthetic derivative of the podophyllotoxins). It inhibits DNA topoisomerase II, thereby ultimately inhibiting DNA synthesis. Etoposide is cell cycle dependent and phase specific, affecting mainly the S and G2 phases. Two different dose-dependent responses are seen. At high concentrations (10 µg/mL or more), lysis of cells entering mitosis is observed. At low concentrations (0.3 to 10 µg/mL), cells are inhibited from entering prophase. It does not interfere with microtubular assembly. The predominant macromolecular effect of etoposide appears to be the induction of DNA strand breaks by an interaction with DNA-topoisomerase II or the formation of free radicals. |
Targets
| Target | Organism | Actions |
|---|---|---|
| DNA topoisomerase 2-alpha | Humans | inhibitor |
| DNA topoisomerase 2-beta | Humans | inhibitor |
ADME / PK
| Absorption | Absorbed well, time to peak plasma concentration is 1-1.5 hrs. Mean bioavailability is 50% (range of 25% - 75%). Cmax and AUC values for orally administered etoposide capsules display intra- and inter-subject variability. There is no evidence of first-pass effect for etoposide. |
|---|---|
| Half-life | 4-11 hours |
| Protein binding | 97% protein bound. |
| Metabolism | Primarily hepatic (through O-demethylation via the CYP450 3A4 isoenzyme pathway) with 40% excreted unchanged in the urine. Etoposide also undergoes glutathione and glucuronide conjugation which are catalyzed by GSTT1/GSTP1 and UGT1A1, respectively. Prostaglandin synthases are also responsible for the conversion of etoposide to O-demethylated metabolites (quinone). |
| Route of elimination | Etoposide is cleared by both renal and nonrenal processes, i.e., metabolism and biliary excretion. Glucuronide and/or sulfate conjugates of etoposide are also excreted in human urine. Biliary excretion of unchanged drug and/or metabolites is an important route of etoposide elimination as fecal recovery of radioactivity is 44% of the intravenous dose. 56% of the dose was in the urine, 45% of which was excreted as etoposide. |
| Volume of distribution | The disposition of etoposide is a biphasic process with a distribution half-life of 1.5 hours. It does not cross into cerebrospinal fluid well. Volume of distribution, steady state = 18 - 29 L. |
| Clearance | * Total body clearance = 33 - 48 mL/min [IV administration, adults] * Mean renal clearance = 7 - 10 mL/min/m^2 |
Formulation & handling
- Etoposide is available in both oral capsule and intravenous injectable formulations requiring attention to route-specific stability and dosing considerations.
- As a small molecule podophyllotoxin derivative, etoposide exhibits moderate water solubility with a LogP of 1.16, impacting formulation strategies for solubility enhancement.
- Avoid co-administration with grapefruit products and St. John's Wort due to CYP3A4 interaction risks affecting etoposide metabolism and systemic exposure.
Regulatory status
| Lifecycle | The active pharmaceutical ingredient (API) has a patent expiry date in the United States and Canada within the next 12 months, indicating an approaching transition to generic market competition. Current products containing this API are marketed primarily in both regions, reflecting a mature market stage. |
|---|
| Markets | Canada, US |
|---|
Supply Chain
| Supply chain summary | The manufacturing landscape for Etoposide includes multiple originator and generic pharmaceutical companies, indicating a diverse supply base. Branded products are predominantly present in the US and Canadian markets, reflecting global distribution primarily concentrated in North America. Patent expirations have likely enabled existing generic competition, as evidenced by numerous manufacturers and packagers offering the drug. |
|---|
Safety
| Toxicity | Side effects include alopecia, constipation, diarrhea, nausea and vomiting and secondary malignancies (leukemia). |
|---|
- Exposure may cause gastrointestinal disturbances including nausea, vomiting, diarrhea, and constipation
- Potential for secondary malignancies such as leukemia has been observed with prolonged exposure
- Handle with appropriate protective equipment to minimize risk of systemic toxicity and contact-related adverse effects
Etoposide is a type of Cytostatic antibiotics
Cytostatic antibiotics are a subcategory of pharmaceutical active pharmaceutical ingredients (APIs) that play a crucial role in the treatment of various types of cancer. These antibiotics possess powerful cytostatic or cell-inhibiting properties, which impede the growth and division of cancer cells.
Cytostatic antibiotics work by selectively targeting and inhibiting specific enzymes and proteins necessary for the replication and proliferation of cancer cells. By interrupting these vital cellular processes, these APIs effectively hinder the progression of cancer and prevent the spread of malignant cells.
One prominent example of a cytostatic antibiotic is Doxorubicin, which belongs to the anthracycline class of antibiotics. Doxorubicin functions by intercalating with DNA molecules, preventing DNA replication and inhibiting the activity of topoisomerase enzymes. These mechanisms effectively impede the growth and division of cancer cells.
Another commonly used cytostatic antibiotic is Mitomycin C. It exerts its anticancer effects by inducing DNA cross-linking, leading to the inhibition of DNA synthesis and cell division. This antibiotic is particularly effective against a variety of solid tumors.
Cytostatic antibiotics are administered in different ways, such as intravenous injection or oral consumption, depending on the specific drug. These APIs are often used in combination with other chemotherapy agents or treatment modalities to achieve optimal therapeutic outcomes.
In conclusion, cytostatic antibiotics are a vital subcategory of pharmaceutical APIs used in cancer treatment. Their ability to inhibit cell growth and division makes them essential in combating various types of cancer, ultimately improving patient outcomes.
Etoposide (Cytostatic antibiotics), 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.
Etoposide API manufacturers & distributors
Compare qualified Etoposide API suppliers worldwide. We currently have 6 companies offering Etoposide 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 |
|---|---|---|---|---|---|
| Adley Formulations | Producer | India | India | CoA, GMP | 14 products |
| Cipla | Producer | India | India | CEP, CoA, FDA, GMP, USDMF, WC | 164 products |
| Justesa Imagen | Producer | Spain | Spain | CoA, GMP | 15 products |
| Nippon Kayaku | Producer | Japan | Japan | CEP, CoA, FDA, GMP, USDMF | 6 products |
| Shanghai Jinhe Bio-Pharma | Producer | China | China | CoA | 12 products |
| Sicor | Producer | Italy | Italy | CoA, GMP | 47 products |
When sending a request, specify which Etoposide 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.).
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