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Imatinib | CAS No: 152459-95-5 | GMP-certified suppliers
A medication that supports treatment of Philadelphia chromosome–positive leukemias, malignant gastrointestinal stromal tumors, and selected myeloproliferative or solid tumor conditions across key global markets.
Therapeutic categories
Primary indications
- Imatinib is indicated for the treatment of adult and pediatric chronic myeloid leukemia with Philadelphia chromosome mutation (Ph+) in blast crisis, accelerated phase, or chronic phase after IFN-alpha therapy failure
- Additionally, imatinib is also indicated to treat adult and pediatric Ph+ acute lymphoblastic leukemia, adult myelodysplastic/myeloproliferative diseases, adult aggressive systemic mastocytosis, adult hypereosinophilic syndrome and/or chronic eosinophilic leukemia (CEL), adult dermatofibrosarcoma protuberans, and malignant gastrointestinal stromal tumors (GIST)
Product Snapshot
- Imatinib is an oral small‑molecule tyrosine kinase inhibitor supplied mainly as tablets and capsules
- It is used in a range of hematologic malignancies including Ph+ CML and ALL, as well as GIST and other specified myeloproliferative or solid tumor indications
- It is approved in major regulated markets including the US, EU, and Canada
Clinical Overview
The pharmacologic activity of imatinib derives from potent inhibition of the BCR‑ABL fusion kinase, which drives dysregulated proliferation and impaired apoptosis in Philadelphia chromosome–positive malignancies. By occupying the ATP‑binding site of BCR‑ABL, imatinib prevents phosphorylation of downstream signaling proteins involved in Ras/MAPK, Src/Pax/Fak/Rac, and PI3K/AKT pathways. Normal cells rely on redundant kinases, contributing to the observed selectivity for malignant cells. Imatinib also inhibits c‑Kit and platelet‑derived growth factor receptors, supporting its activity in gastrointestinal stromal tumors and certain myeloproliferative conditions.
Imatinib is orally administered with high bioavailability and is extensively metabolized hepatically, predominantly by CYP3A isoforms. It is a substrate and inhibitor of multiple CYP enzymes and transporters, creating potential for clinically relevant drug–drug interactions. Elimination occurs mainly via fecal excretion of metabolites. Protein binding is high, and steady‑state concentrations are reached within approximately one week of daily dosing.
Key safety considerations include myelosuppression, hepatotoxicity, fluid retention, gastrointestinal effects, and rare cardiotoxicity. QTc prolongation risk warrants caution with concurrent QT‑prolonging agents. As both a substrate and inhibitor of several CYP450 enzymes and efflux transporters, careful medication reconciliation is essential.
Imatinib is marketed in many regions as imatinib mesylate. For API procurement, sourcing should emphasize compliance with current Good Manufacturing Practice, robust impurity control for kinase inhibitor–specific degradation pathways, and reliable documentation supporting global regulatory submissions.
Identification & chemistry
| Generic name | Imatinib |
|---|---|
| Molecule type | Small molecule |
| CAS | 152459-95-5 |
| UNII | BKJ8M8G5HI |
| DrugBank ID | DB00619 |
Pharmacology
| Summary | Imatinib is a small‑molecule tyrosine kinase inhibitor that targets the BCR‑ABL fusion protein driving aberrant signaling in Philadelphia chromosome–positive malignancies. It binds the ATP‑binding site of BCR‑ABL and also inhibits other receptor tyrosine kinases such as c‑Kit and PDGF receptors, disrupting pathways involved in proliferation, survival, and motility. These actions reduce growth and promote apoptosis in tumor cells dependent on these signaling networks. |
|---|---|
| Mechanism of action | Imatinib mesylate is a protein-tyrosine kinase inhibitor that inhibits the BCR-ABL tyrosine kinase, the constitutively active tyrosine kinase created by the Philadelphia chromosome abnormality in CML.Although the function of normal BCR is still unclear, ABL activation is overexpressed in various tumors and is heavily implicated in cancer cells growth and survival.Imatinib inhibits the BCR-ABL protein by binding to the ATP pocket in the active site, thus preventing downstream phosphorylation of target protein. Imatinib is also an inhibitor of the receptor tyrosine kinases for platelet-derived growth factor (PDGF) and stem cell factor (SCF), c-Kit, and inhibits PDGF- and SCF-mediated cellular events. In vitro, imatinib inhibits proliferation and induces apoptosis in GIST cells, which express an activating c-Kit mutation. |
| Pharmacodynamics | Imatinib is a 2-phenylaminopyrimidine derivative neoplastic agent that belongs to the class of tyrosine kinase inhibitors.Although imatinib inhibits a number of tyrosine kinases, it is quite selective toward the BCR-ABL fusion protein that is present in various cancers.BCR-ABL pathway controls many downstream pathways that are heavily implicated in neoplastic growth such as the Ras/MapK pathway (cellular proliferation), Src/Pax/Fak/Rac pathway (cellular motility), and PI/PI3K/AKT/BCL-2 pathway (apoptosis pathway).Therefore, the BCR-ABL pathway is an attractive target for cancer treatment. Although normal cells also depend on these pathways for growth, these cells tend to have redundant tyrosine kinases to continually function in spite of ABL inhibition from imatinib.Cancer cells, on the other hand, can have a dependence on BCR-ABL, thus more heavily impacted by imatinib. |
Targets
| Target | Organism | Actions |
|---|---|---|
| Breakpoint cluster region protein | Humans | inhibitor |
| Mast/stem cell growth factor receptor Kit | Humans | antagonist |
| Proto-oncogene tyrosine-protein kinase receptor Ret | Humans | inhibitor |
ADME / PK
| Absorption | Imatinib is well absorbed after oral administration with Cmax achieved within 2-4 hours post-dose. Mean absolute bioavailability is 98%.Mean imatinib AUC increases proportionally with increasing doses ranging from 25 mg to 1,000 mg.There is no significant change in the pharmacokinetics of imatinib on repeated dosing, and accumulation is 1.5- to 2.5-fold at a steady state when Gleevec is dosed once daily. |
|---|---|
| Half-life | Following oral administration in healthy volunteers, the elimination half-lives of imatinib and its major active metabolite, the N-desmethyl derivative (CGP74588), are approximately 18 and 40 hours, respectively. |
| Protein binding | At clinically relevant concentrations of imatinib, binding to plasma proteins in in vitro experiments is approximately 95%, mostly to albumin and α1-acid glycoprotein. |
| Metabolism | CYP3A4 is the major enzyme responsible for the metabolism of imatinib. Other cytochrome P450 enzymes, such as CYP1A2, CYP2D6, CYP2C9, and CYP2C19, play a minor role in its metabolism. The main circulating active metabolite in humans is the N-demethylated piperazine derivative, formed predominantly by CYP3A4. It shows in vitro potency similar to the parent imatinib. |
| Route of elimination | Imatinib elimination is predominately in the feces, mostly as metabolites. Based on the recovery of compound(s) after an oral 14C-labeled dose of imatinib, approximately 81% of the dose was eliminated within 7 days, in feces (68% of dose) and urine (13% of dose).Unchanged imatinib accounted for 25% of the dose (5% urine, 20% feces), the remainder being metabolites. |
| Volume of distribution | Population pharmacokinetics in adult CML patients estimated the steady-state volume of distribution of imatinib to be 295.0 ± 62.5 L.At a dose of 340 mg/m<sup>2</sup>, the volume of distribution of imatinib in pediatric patients was calculated to be 167 ± 84 L. |
| Clearance | Typically, clearance of imatinib in a 50-year-old patient weighing 50 kg is expected to be 8 L/h, while for a 50-year-old patient weighing 100 kg the clearance will increase to 14 L/h. The inter-patient variability of 40% in clearance does not warrant initial dose adjustment based on body weight and/or age but indicates the need for close monitoring for treatment-related toxicities. |
Formulation & handling
- Low aqueous solubility and relatively high lipophilicity drive the need for solubilization or solid‑dispersion strategies in oral formulations.
- As an oral small‑molecule solid, it is typically formulated as film‑coated tablets or capsules to improve swallowability and limit gastric irritation.
- Food can influence gastric tolerability, so formulations may account for administration with meals without relying on pH‑dependent release mechanisms.
Regulatory status
| Lifecycle | Most patent protection for the API has lapsed, with expiry occurring in Canada in 2013 and in the United States between 2019 and 2022, indicating a mature lifecycle. With products marketed in Canada, the US, and the EU, the API is positioned in well‑established markets where generic competition is likely present or emerging. |
|---|
| Markets | Canada, US, EU |
|---|
Supply Chain
| Supply chain summary | Imatinib is led by a single originator manufacturer, with several secondary packagers supporting distribution. Branded products are established across the US, EU, and Canada, indicating broad global availability. Key patents in major markets have expired, enabling established generic competition. |
|---|
Safety
| Toxicity | The most frequently reported adverse reactions (>30%) were edema, nausea, vomiting, muscle cramps, musculoskeletal pain, diarrhea, rash, fatigue and abdominal pain. In the 2-year rat carcinogenicity study administration of imatinib at 15, 30, and 60 mg/kg/day resulted in a statistically significant reduction in the longevity of males at 60 mg/kg/day and females at greater than or equal to 30 mg/kg/day. Target organs for neoplastic changes were the kidneys (renal tubule and renal pelvis), urinary bladder, urethra, preputial and clitoral gland, small intestine, parathyroid glands, adrenal glands, and non-glandular stomach. Neoplastic lesions were not seen at 30 mg/kg/day for the kidneys, urinary bladder, urethra, small intestine, parathyroid glands, adrenal glands, and non-glandular stomach, and 15 mg/kg/day for the preputial and clitoral gland. The papilloma/carcinoma of the preputial/clitoral gland was noted at 30 and 60 mg/kg/day, representing approximately 0.5 to 4 or 0.3 to 2.4 times the human daily exposure (based on AUC) at 400 mg/day or 800 mg/day, respectively, and 0.4 to 3.0 times the daily exposure in children (based on AUC) at 340 mg/m2. The renal tubule adenoma/carcinoma, renal pelvis transitional cell neoplasms, the urinary bladder and urethra transitional cell papillomas, the small intestine adenocarcinomas, the parathyroid glands adenomas, the benign and malignant medullary tumors of the adrenal glands and the non-glandular stomach papillomas/carcinomas were noted at 60 mg/kg/day. The relevance of these findings in the rat carcinogenicity study for humans is not known. Positive genotoxic effects were obtained for imatinib in an in vitro mammalian cell assay (Chinese hamster ovary) for clastogenicity (chromosome aberrations) in the presence of metabolic activation. Two intermediates of the manufacturing process, which are also present in the final product, are positive for mutagenesis in the Ames assay. One of these intermediates was also positive in the mouse lymphoma assay. Imatinib was not genotoxic when tested in an in vitro bacterial cell assay (Ames test), an in vitro mammalian cell assay (mouse lymphoma) and an in vivo rat micronucleus assay. In a study of fertility, male rats were dosed for 70 days prior to mating and female rats were dosed 14 days prior to mating and through to gestational Day 6. Testicular and epididymal weights and percent motile sperm were decreased at 60 mg/kg, approximately three-fourths the maximum clinical dose of 800 mg/day based on BSA. This was not seen at doses less than or equal to 20 mg/kg (one-fourth of the maximum human dose of 800 mg). The fertility of male and female rats was not affected. Fertility was not affected in the preclinical fertility and early embryonic development study although lower testes and epididymal weights, as well as a reduced number of motile sperm, were observed in the high-dose male rats. In the preclinical pre-and postnatal study in rats, fertility in the first generation offspring was also not affected by imatinib mesylate. It is important to consider potential toxicities suggested by animal studies, specifically, liver, kidney, and cardiac toxicity and immunosuppression. Severe liver toxicity was observed in dogs treated for 2 weeks, with elevated liver enzymes, hepatocellular necrosis, bile duct necrosis, and bile duct hyperplasia. Renal toxicity was observed in monkeys treated for 2 weeks, with focal mineralization and dilation of the renal tubules and tubular nephrosis. Increased blood urea nitrogen (BUN) and creatinine were observed in several of these animals. An increased rate of opportunistic infections was observed with chronic imatinib treatment in laboratory animal studies. In a 39-week monkey study, treatment with imatinib resulted in the worsening of normally suppressed malarial infections in these animals. Lymphopenia was observed in animals (as in humans). Additional long-term toxicities were identified in a 2-year rat study. Histopathological examination of the treated rats that died in the study revealed cardiomyopathy (both sexes), chronic progressive nephropathy (females), and preputial gland papilloma as principal causes of death or reasons for sacrifice. Non-neoplastic lesions seen in this 2-year study that were not identified in earlier preclinical studies were the cardiovascular system, pancreas, endocrine organs, and teeth. The most important changes included cardiac hypertrophy and dilatation, leading to signs of cardiac insufficiency in some animals. |
|---|
- High incidence (›30%) of edema, GI disturbances, musculoskeletal symptoms, and fatigue reported in clinical toxicity profiles
- Handling should account for potential irritant or sensitizing characteristics
- Animal studies indicate multi‑organ toxicities at elevated exposures, including hepatic necrosis, renal tubular injury, cardiac hypertrophy, and immunosuppression, with documented neoplastic findings in rats at higher dose levels
US Drug Master File (USDMF)
A US Drug Master File (USDMF) is a confidential document submitted to the U.S. Food and Drug Administration (FDA) that provides detailed information about the manufacturing process of an Active Pharmaceutical Ingredient (API) or a finished pharmaceutical product. This document includes comprehensive details such as chemical properties, manufacturing facilities, production processes, packaging specifications, storage conditions, and more.
The USDMF ensures that proprietary information remains protected while allowing the FDA to review the data as part of drug approval processes. Unlike other types of DMFs used in different regions, the USDMF is specifically designed to meet the regulatory requirements set by the FDA, ensuring compliance with U.S. standards.
Imatinib Mesylate is a type of Protein kinase inhibitors
Protein kinase inhibitors are a vital subcategory of pharmaceutical active pharmaceutical ingredients (APIs) that play a crucial role in targeted cancer therapies. These inhibitors specifically target and block the activity of protein kinases, enzymes that regulate various cellular processes, including cell growth, division, and signal transduction.
Protein kinase inhibitors function by binding to the active site of protein kinases, preventing them from phosphorylating specific proteins and disrupting intracellular signaling pathways. This targeted approach inhibits the uncontrolled growth and proliferation of cancer cells, ultimately leading to their death.
The development of protein kinase inhibitors has revolutionized cancer treatment by providing more effective and less toxic alternatives to traditional chemotherapy. These drugs have demonstrated impressive results in the treatment of various cancers, including lung, breast, and leukemia.
The pharmaceutical industry invests heavily in research and development to discover novel protein kinase inhibitors with improved potency, selectivity, and pharmacokinetic properties. High-throughput screening, computational modeling, and structure-activity relationship studies are employed to identify potential lead compounds.
The success of protein kinase inhibitors in treating cancer has spurred significant interest in this subcategory of APIs. Ongoing research aims to expand their applications to other diseases, such as autoimmune disorders and neurological conditions.
In conclusion, protein kinase inhibitors are a valuable class of pharmaceutical APIs with immense potential for targeted cancer therapies. Continued advancements in this field hold promise for improved treatment outcomes and enhanced patient care.
Imatinib Mesylate (Protein kinase inhibitors), 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.
Imatinib Mesylate API manufacturers & distributors
Compare qualified Imatinib Mesylate API suppliers worldwide. We currently have 28 companies offering Imatinib Mesylate API, with manufacturing taking place in 9 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 |
|---|---|---|---|---|---|
| Acebright Pharma | Producer | India | India | CoA, USDMF | 9 products |
| Adley Formulations | Producer | India | India | CoA, GMP | 14 products |
| AXXO GmbH | Distributor | Germany | European Union | CoA, GMP, GDP, MSDS | 243 products |
| Cipla | Producer | India | Unknown | CEP, CoA, FDA, GMP, KDMF, USDMF, WC | 164 products |
| Flavine | Distributor | Germany | Unknown | CoA | 83 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 |
| Gonane Pharma | Producer | India | India | GMP | 166 products |
| Hetero Labs | Producer | India | India | CEP, CoA, GMP, JDMF, USDMF, WC | 90 products |
| Ind-Swift Labs. | Producer | India | India | CoA, FDA, GMP, WC | 27 products |
| Intas Pharma | Producer | United Kingdom | Unknown | CoA, USDMF | 30 products |
| Laurus Labs | Producer | India | India | CEP, CoA, GMP, USDMF, WC | 50 products |
| LGM Pharma | Distributor | United States | World | BSE/TSE, CEP, CoA, GMP, MSDS, USDMF | 441 products |
| MSN Labs. | Producer | India | India | CEP, CoA, GMP, USDMF, WC | 119 products |
| Natco Pharma | Producer | India | India | CEP, CoA, FDA, GMP, JDMF, KDMF, USDMF, WC | 40 products |
| PLIVA | Producer | Czech Republic | Czech Republic | CoA, JDMF | 31 products |
| Qilu Tianhe | Producer | China | China | CEP, CoA, GMP, USDMF, WC | 16 products |
| Reliance Life Sciences | Producer | India | India | CoA, USDMF, WC | 11 products |
| Senova Technology Co., Lt... | Producer | China | China | CoA, GMP, ISO9001, USDMF | 157 products |
| SETV Global | Producer | India | India | CoA, FDA, GMP | 515 products |
| Shaoxing Hantai Pharma | Distributor | China | China | CoA | 162 products |
| Shilpa Medicare Ltd | Producer | India | India | BSE/TSE, CEP, CoA, EDMF/ASMF, GMP, ISO9001, MSDS, USDMF, WC | 54 products |
| Shin Poong Pharm | Producer | South Korea | South Korea | CoA, JDMF | 11 products |
| Signa | Producer | Mexico | Mexico | CEP, CoA, FDA, USDMF | 42 products |
| Sinoway industrial Co.,Lt... | Distributor | China | China | CEP, CoA, GMP, ISO9001, MSDS, USDMF | 764 products |
| Sumitomo Chemical | Producer | Japan | Japan | CoA, JDMF | 28 products |
| Sun Pharma | Producer | India | India | CoA, GMP, USDMF, WC | 219 products |
| Zhejiang Hisun Pharma | Producer | China | China | CoA, USDMF | 69 products |
When sending a request, specify which Imatinib Mesylate 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 Imatinib Mesylate 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.
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