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Ponatinib | CAS No: 943319-70-8 | GMP-certified suppliers
A medication that treats resistant or intolerant chronic myeloid leukemia and Philadelphia chromosome-positive acute lymphoblastic leukemia by targeting multiple tyrosine kinases for antineoplastic therapy.
Therapeutic categories
Primary indications
- Ponatinib is indicated for the treatment of adult patients with chronic phase, accelerated phase, or blast phase chronic myeloid leukemia (CML) that is resistant or intolerant to prior tyrosine kinase inhibitor therapy or Philadelphia chromosome positive acute lymphoblastic leukemia (Ph+ALL) that is resistant or intolerant to prior tyrosine kinase inhibitor therapy
Product Snapshot
- Ponatinib is an oral small molecule formulated as film-coated tablets
- It is primarily used for resistant or intolerant cases of chronic myeloid leukemia (CML) and Philadelphia chromosome positive acute lymphoblastic leukemia (Ph+ALL)
- Ponatinib is approved for use in major regulatory markets including the United States, Canada, and the European Union
Clinical Overview
Ponatinib belongs to the chemical class of benzanilides, characterized by an anilide group linked to a benzene ring. Its mechanism of action involves multi-kinase inhibition, predominantly targeting the Bcr-Abl tyrosine kinase protein. Beyond Abl and its T315I mutant form, ponatinib inhibits several other receptor tyrosine kinases including VEGFR, PDGFR, FGFR, EPH receptors, SRC family kinases, KIT, RET, TIE2, and FLT3, contributing to its broad antineoplastic effects. Preclinical models have demonstrated tumor size reduction in cells expressing native or T315I-mutant Bcr-Abl.
Pharmacokinetic data show ponatinib is a substrate for cytochrome P450 enzymes CYP3A4, CYP2C8, and CYP2D6, all relevant for its metabolism, alongside interactions with P-glycoprotein transport mechanisms. The compound has a narrow therapeutic index, necessitating careful dose management to mitigate toxicities. Reported safety concerns include hepatotoxicity and myelosuppression, which require monitoring in clinical use.
Ponatinib is classified among antineoplastic agents, kinase inhibitors, and immunomodulating agents with a complex metabolic profile. Quality considerations during active pharmaceutical ingredient (API) procurement should prioritize stringent control of purity, absence of genotoxic impurities, and consistent polymorphic form, given its narrow therapeutic index and role in critical oncology treatments. Reliable sourcing from GMP-compliant manufacturers and comprehensive analytical characterization are essential to ensure API suitability for formulation and regulatory submission.
Identification & chemistry
| Generic name | Ponatinib |
|---|---|
| Molecule type | Small molecule |
| CAS | 943319-70-8 |
| UNII | 4340891KFS |
| DrugBank ID | DB08901 |
Pharmacology
| Summary | Ponatinib is a multi-target kinase inhibitor primarily targeting the Bcr-Abl tyrosine kinase, including its T315I mutant form associated with resistance in chronic myeloid leukemia (CML). It also inhibits several receptor tyrosine kinases involved in angiogenesis and cell proliferation, such as VEGFR, PDGFR, FGFR, KIT, RET, and FLT3. Ponatinib’s pharmacodynamic effects include suppression of aberrant kinase signaling pathways contributing to hematologic malignancies resistant to prior tyrosine kinase inhibitor therapies. |
|---|---|
| Mechanism of action | Ponatinib is a multi-target kinase inhibitor. Its primary cellular target is the Bcr-Abl tyrosine kinase protein which is constitutively active and promotes the progression of CML. This protein arises from the fused Bcr and Abl gene- what is commonly known as the Philadelphia chromosome. Ponatinib is unique in that it is especially useful in the treatment of resistant CML because it inhibits the tyrosine kinase activity of Abl and T315I mutant kinases. The T315I mutation confers resistance in cells as it prevents other Bcr-Abl inhibitors from binding to the Abl kinase. Other targets that ponatinib inhibits are members of the VEGFR, PDGFR, FGFR, EPH receptors and SRC families of kinases, and KIT, RET, TIE2, and FLT3. A decrease in tumour size expressing native or T315I mutant BCR-ABL have been observed in rats. |
Targets
| Target | Organism | Actions |
|---|---|---|
| Tyrosine-protein kinase ABL1 | Humans | inhibitor |
| Breakpoint cluster region protein | Humans | inhibitor |
| Mast/stem cell growth factor receptor Kit | Humans | inhibitor |
ADME / PK
| Absorption | The absolute bioavailability of ponatinib is unknown. Peak concentrations of ponatinib are observed within 6 hours after Iclusig oral administration. Food does not affect absorption of food. The aqueous solubility of ponatinib is pH dependent, with higher pH resulting in lower solubility. When 45 mg of ponatinib is given to cancer patients, the pharmacokinetic parameters are as follows: Cmax = 73 ng/mL; AUC = 1253 ng•hr/mL; |
|---|---|
| Half-life | After oral administration of 45 mg ponatinib once daily for 28 days in cancer patients, the terminal elimination half-life is 24 hours (range of 12 - 66 hours). |
| Protein binding | > 99% bound to plasma proteins. |
| Metabolism | At least 64% of a ponatinib dose undergoes phase I and phase II metabolism. CYP3A4 and to a lesser extent CYP2C8, CYP2D6 and CYP3A5 are involved in the phase I metabolism of ponatinib in vitro. Ponatinib is also metabolized by esterases and/or amidases. |
| Route of elimination | Ponatinib is mainly eliminated via feces. Following a single oral dose of [14C]-labeled ponatinib, approximately 87% of the radioactive dose is recovered in the feces and approximately 5% in the urine. |
| Volume of distribution | After oral administration of 45 mg ponatinib once daily for 28 days in cancer patients, the steady state volume of distribution is 1223 L. Ponatinib is a weak substrate for P-gp and ABCG2. |
Formulation & handling
- Ponatinib is a small molecule formulated for oral administration as film-coated and coated tablets.
- It exhibits low water solubility and high lipophilicity (LogP 4.97), indicating formulation may require solubilization strategies.
- Caution is advised regarding CYP3A4-mediated drug interactions, particularly with St. John's Wort and grapefruit products, influencing bioavailability.
Regulatory status
| Lifecycle | The API is currently protected by patents in the United States with expirations spanning from late 2026 to late 2033. It is marketed in the US, Canada, and the EU, indicating varying stages of market maturity across these regions. |
|---|
| Markets | US, Canada, EU |
|---|
Supply Chain
| Supply chain summary | Ponatinib is supplied primarily by a limited number of originator companies with branded products marketed in the US, Canada, and EU. Multiple patents protect the compound in the United States, with key expirations starting in late 2026 and extending through 2033. These patent timelines indicate that generic competition may emerge in the mid- to long-term future, but currently branded exclusivity persists. |
|---|
Safety
| Toxicity | The most common non-hematologic adverse reactions (≥ 20%) were hypertension, rash, abdominal pain, fatigue, headache, dry skin, constipation, arthralgia, nausea, and pyrexia. Hematologic adverse reactions included thrombocytopenia, anemia, neutropenia, lymphopenia, and leukopenia. |
|---|
- Handle with appropriate personal protective equipment to minimize exposure, as the compound is associated with hematologic toxicities including thrombocytopenia and neutropenia
- Avoid inhalation and skin contact due to potential for systemic adverse effects such as hypertension, rash, and fatigue
- Implement control measures to prevent environmental release, considering the compound's toxicity profile indicating multiple organ system effects
Ponatinib 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.
Ponatinib (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.
Ponatinib API manufacturers & distributors
Compare qualified Ponatinib API suppliers worldwide. We currently have 1 companies offering Ponatinib API, with manufacturing taking place in 1 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 |
|---|---|---|---|---|---|
| Sichuan Qingmu Pharmaceut... | Producer | China | China | CoA | 31 products |
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