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Idelalisib | CAS No: 870281-82-6 | GMP-certified suppliers
A medication that treats chronic lymphocytic leukemia, relapsed follicular B-cell non-Hodgkin lymphoma, and relapsed small lymphocytic lymphoma, offering targeted therapy for specific hematologic malignancies.
Therapeutic categories
Primary indications
- Idelalisib is indicated in the treatment of chronic lymphocytic leukemia (CLL), relapsed follicular B-cell non-Hodgkin lymphoma (FL), and relapsed small lymphocytic lymphoma (SLL)
- For the treatment of relapsed CLL, it is currently indicated as a second-line agent in combination with rituximab in patients for whom rituximab alone would be considered appropriate therapy due to other co-morbidities, while in the treatment of FL and SLL it is intended to be used in patients who have received at least two prior systemic therapies
Product Snapshot
- Idelalisib is an oral small molecule formulation available as film-coated tablets
- It is primarily used for the treatment of chronic lymphocytic leukemia, relapsed follicular B-cell non-Hodgkin lymphoma, and relapsed small lymphocytic lymphoma
- The product is approved in key regulatory markets including the US, Canada, and the EU
Clinical Overview
Pharmacologically, idelalisib selectively inhibits the p110δ isoform of class IA PI3Ks. This enzyme is predominantly expressed in leukocytes and plays a critical role in signal transduction pathways governing cell proliferation, survival, differentiation, and motility. By targeting p110δ, idelalisib interferes with B-cell receptor (BCR) signaling and chemokine receptor pathways, including those mediated by CXCR4 and CXCR5, which regulate the homing and trafficking of malignant B cells to the lymph nodes and bone marrow. The inhibition of these pathways results in apoptosis and reduced viability of malignant lymphoid cells.
In terms of drug metabolism and pharmacokinetics, idelalisib is a substrate and modulator of multiple cytochrome P450 enzymes, notably CYP3A4, CYP2C19, CYP2C8, and CYP2B6 isoforms. It also interacts with transport proteins such as P-glycoprotein and organic anion-transporting polypeptides (OATP1B1 and OATP1B3). These interactions necessitate careful consideration of potential drug-drug interactions during clinical use due to its narrow therapeutic index. Metabolism involves UGT1A4-mediated pathways, with idelalisib acting as both substrate and inhibitor of this enzyme.
Safety profiles indicate idelalisib is associated with hepatotoxicity and immunosuppressive effects, warranting monitoring of liver function and careful management to avoid severe infections. Due to its mechanism targeting immune cell signaling, caution is advised in patients with concurrent immune compromise.
Idelalisib is classified chemically as a 6-alkylaminopurine derivative. It is marketed under various regulatory approvals as a kinase inhibitor with immunomodulatory and antineoplastic activity.
For API procurement, attention to synthesis reproducibility, purity profile, and control of related impurities is critical given the complexity of the molecule and its involvement with multiple enzymatic pathways. Compliance with regulatory guidelines for antineoplastic agents and confirmation of batch consistency through validated analytical methods should be prioritized to ensure therapeutic quality and safety.
Identification & chemistry
| Generic name | Idelalisib |
|---|---|
| Molecule type | Small molecule |
| CAS | 870281-82-6 |
| UNII | YG57I8T5M0 |
| DrugBank ID | DB09054 |
Pharmacology
| Summary | Idelalisib is a selective inhibitor of the delta isoform of phosphatidylinositol 3-kinase (PI3Kδ), an enzyme predominantly expressed in leukocytes and involved in key signaling pathways regulating cell growth, survival, and migration. By targeting PI3Kδ, idelalisib disrupts B-cell receptor and chemokine receptor signaling, leading to apoptosis of malignant B cells and impaired trafficking to lymphoid tissues. It is utilized in the management of certain B-cell malignancies, including chronic lymphocytic leukemia and non-Hodgkin lymphomas. |
|---|---|
| Mechanism of action | Idelalisib specifically inhibits P110δ, the delta isoform of the enzyme phosphatidylinositol-4,5-bisphosphate 3-kinase, also known as PI-3K. The PI-3Ks are a family of enzymes involved in cellular functions such as cell growth, proliferation, differentiation, motility, survival and intracellular trafficking, which in turn are involved in cancer. In contrast to the other class IA PI3Ks p110α and p110β, p110δ is principally expressed in leukocytes (white blood cells) and is important for the function of T cells, B cell, mast cells and neutrophils. By inhibiting this enzyme, idelalisib induces apoptosis of malignant cells and inhibits several cell signaling pathways, including B-cell receptor (BCR) signaling and C-X-C chemokine receptors type 5 and type 4 signalling, which are involved in trafficking and homing of B-cells to the lymph nodes and bone marrow. Treatment of lymphoma cells with idelalisib has been shown to result in inhibition of chemotaxis and adhesion, and reduced cell viability. |
Targets
| Target | Organism | Actions |
|---|---|---|
| Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform | Humans | inhibitor |
ADME / PK
| Absorption | Following oral administration, the median Tmax was observed at 1.5 hours. |
|---|---|
| Half-life | The terminal elimination half-life is 8.2 hours. |
| Protein binding | Idelalisib is greater than 84% bound to human plasma proteins with no concentration dependence. |
| Metabolism | Idelalisib is metabolized by aldehyde oxidase and CYP3A to its major metabolite GS-563117, which is inactive against P110δ. Idelalisib is also metabolized to a minor extent by UGT1A4. |
| Route of elimination | Following a single dose of 150 mg of [14C] idelalisib, 78% and 14% of the radioactivity was excreted in feces and urine, respectively. GS-563117, idelalisib's major metabolite, accounted for 49% of the radioactivity in the urine and 44% in the feces. |
| Volume of distribution | 23 L |
| Clearance | 14.9 L/hr |
Formulation & handling
- Idelalisib is a small molecule oral agent available in tablet form, including film-coated formulations.
- Avoid concurrent use of grapefruit products and St. John's Wort due to significant CYP3A-mediated drug interaction risks.
- Stable for oral administration with no strict food requirements, though high-fat meals may moderately increase systemic exposure.
Regulatory status
| Lifecycle | The API is present in mature markets including the US, Canada, and the EU, with key US patents expiring between 2021 and 2025, indicating ongoing patent protection has recently lapsed or will soon lapse. This suggests a transition phase toward increased generic competition in these regions. |
|---|
| Markets | US, Canada, EU |
|---|
Supply Chain
| Supply chain summary | Idelalisib is primarily supplied by originator companies holding multiple patents in the United States, with branded products marketed under the name Zydelig across the US, Canada, and the EU. The key patents have expiration dates ranging from 2021 to 2025, indicating a potential or existing opportunity for generic competition, especially following the earlier patent expiries in 2021. The supply landscape is characterized by established patent protection in the US and a broad geographic presence of branded formulations. |
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Idelalisib 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.
Idelalisib (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.
Idelalisib API manufacturers & distributors
Compare qualified Idelalisib API suppliers worldwide. We currently have 3 companies offering Idelalisib API, with manufacturing taking place in 3 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 |
|---|---|---|---|---|---|
| LGM Pharma | Distributor | United States | World | BSE/TSE, CEP, CoA, GMP, MSDS, USDMF | 441 products |
| Lupin | Producer | India | India | CoA, USDMF | 155 products |
| Zhejiang Neo-Dankong | Producer | China | China | CoA, USDMF | 8 products |
When sending a request, specify which Idelalisib 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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