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Lenalidomide | CAS No: 191732-72-6 | GMP-certified suppliers
A medication that treats multiple myeloma, certain myelodysplastic syndromes, and relapsed lymphomas by providing immunomodulatory and antineoplastic benefits.
Therapeutic categories
Primary indications
- Lenalidomide is indicated for the treatment of adult patients with multiple myeloma (MM) in combination with dexamethasone
- It is also indicated as maintenance therapy in multiple myeloma following autologous hematopoietic stem cell transplantation (auto-HSCT)
- It is indicated for the treatment of adult patients with transfusion-dependent anemia due to low- or intermediate-1-risk myelodysplastic syndromes (MDS) associated with a deletion 5q cytogenetic abnormality with or without additional cytogenetic abnormalities
- Lenalidomide is indicated for the treatment of adult patients with mantle cell lymphoma (MCL) whose disease has relapsed or progressed after two prior therapies, one of which included bortezomib
Product Snapshot
- Lenalidomide is an oral small molecule formulation available in coated capsule form
- It is primarily used for the treatment of multiple myeloma, transfusion-dependent anemia in myelodysplastic syndromes, mantle cell lymphoma, and certain types of follicular and marginal zone lymphomas
- Lenalidomide is approved for use in major regulatory markets including the United States, Canada, and the European Union
Clinical Overview
Clinically, lenalidomide is approved by regulatory agencies including the FDA and EMA for multiple hematologic indications. It is indicated in adult patients for the treatment of multiple myeloma in combination with dexamethasone, including as maintenance therapy after autologous hematopoietic stem cell transplantation. Additionally, it is approved for transfusion-dependent anemia in low- or intermediate-1-risk myelodysplastic syndromes with deletion 5q cytogenetic abnormalities. Lenalidomide is also indicated for relapsed or progressive mantle cell lymphoma following at least two prior therapies, and for previously treated follicular and marginal zone lymphomas in combination with rituximab.
Pharmacodynamically, lenalidomide exerts direct cytotoxic effects on hematopoietic malignant cells by promoting apoptosis and inhibiting proliferation. It modulates the tumor microenvironment by inhibiting angiogenesis and reducing inflammatory cytokine levels. It enhances host antitumor immunity by stimulating T cell proliferation and natural killer (NK) cell activity, while increasing antibody-dependent cellular cytotoxicity, especially in combination with anti-CD20 monoclonal antibodies.
Mechanistically, lenalidomide binds cereblon, an E3 ubiquitin ligase substrate receptor, altering substrate specificity to promote degradation of key transcription factors such as Ikaros (IKZF1), Aiolos (IKZF3), and CK1α. This leads to downstream effects on B-cell survival, cytokine production—e.g., increased interleukin-2—and enhanced immune cytotoxicity. It also suppresses pro-inflammatory cytokines and inhibits anti-apoptotic pathways including NF-κB signaling. Anti-angiogenic activity is mediated through inhibition of vascular endothelial growth factor and other growth factors. Additionally, lenalidomide impairs malignant cell adhesion and metastasis-related processes.
Regarding absorption, distribution, metabolism, and excretion (ADME), lenalidomide is administered orally with high bioavailability. It is primarily renally excreted unchanged, and dose adjustments are necessary in patients with renal impairment. It is a substrate for P-glycoprotein but has low hepatic metabolism.
Safety considerations include significant teratogenic risk similar to thalidomide, necessitating strict pregnancy prevention programs such as the Risk Evaluation and Mitigation Strategy (REMS) in the United States. Hematologic toxicities including neutropenia and thrombocytopenia are commonly observed and require monitoring. Other adverse events include thromboembolism, fatigue, and rash.
Notable approved formulations are oral capsules marketed under various brand names globally. In oncology practice, lenalidomide is commonly utilized as a backbone immunomodulatory therapy in combination regimens.
For active pharmaceutical ingredient (API) procurement, considerations include sourcing from manufacturers compliant with Good Manufacturing Practices (GMP) and adherence to stringent quality control standards, given the critical implications of impurities in immunomodulatory agents. Analytical characterization should verify the racemic composition, assay potency, residual solvents, and absence of genotoxic impurities to ensure safety and efficacy in finished pharmaceutical products.
Identification & chemistry
| Generic name | Lenalidomide |
|---|---|
| Molecule type | Small molecule |
| CAS | 191732-72-6 |
| UNII | F0P408N6V4 |
| DrugBank ID | DB00480 |
Pharmacology
| Summary | Lenalidomide is an immunomodulatory agent targeting the cereblon E3 ubiquitin ligase complex to induce ubiquitination and degradation of transcription factors essential for malignant B-cell survival, including IKZF1 and IKZF3. It modulates cytokine production, enhances T cell co-stimulation, and increases natural killer (NK) cell cytotoxicity, contributing to its antineoplastic and anti-inflammatory effects. Additionally, lenalidomide exerts direct antiproliferative and pro-apoptotic effects on tumor cells and inhibits angiogenesis and metastasis by reducing angiogenic factors and disrupting cell adhesion. |
|---|---|
| Mechanism of action | Lenalidomide is a drug with multiple mechanisms of action. Lenalidomide exerts immunomodulating effects by altering cytokine production, regulating T cell co-stimulation, and enhancing the NK cell-mediated cytotoxicity. Lenalidomide directly inhibits the cullin ring E3 ubiquitin ligase complex: upon binding to cereblon, a substrate adaptor of the complex, lenalidomide modulates substrate specificity of the complex to recruit substrate proteins of the ligase, including Ikaros (IKZF1), Aiolos (IKZF3), and CK1α. These substrates are then tagged for ubiquitination and subsequent proteasomal degradation. IKZF1 and IKZF3 are B-cell transcription factors that are essential for B-cell differentiation and survival of malignant cells. IKZF3 also regulates the expression of interferon regulatory factor 4 (IRF4), which is a transcription factor that regulates the aberrant myeloma-specific gene. The immunomodulatory actions of lenalidomide can be partly explained by the degradation of IKZF3, since it is a repressor of the interleukin 2 gene (IL2): as lenalidomide decreases the level of IKZF3, the production of IL-2 increases, thereby increasing the proliferation of natural killer (NK), NKT cells, and CD4+ T cells. Lenalidomide inhibits the production of pro-inflammatory cytokines TNF-α, IL-1, IL-6, and IL-12, while elevating the production of anti-inflammatory cytokine IL-10. Lenalidomide acts as a T-cell co-stimulatory molecule that promotes CD3 T-cell proliferation and increases the production of IL-2 and IFN-γ in T lymphocytes, which enhances NK cell cytotoxicity and ADCC. It inhibits the expression and function of T-regulatory cells, which are often overabundant in some hematological malignancies. Lenalidomide directly exerts antitumour effects by inhibiting the proliferation and inducing apoptosis of tumour cells. Lenalidomide triggers the activation of pro-apoptotic caspase-8, enhances tumour cell sensitivity to FAS-induced apoptosis, and downregulates NF-κB, an anti-apoptotic protein. Independent of its immunomodulatory effects, lenalidomide mediates anti-angiogenic effects by inhibiting angiogenic growth factors released by tumour cells, such as vascular endothelial growth factor (VEGF), basic fibroblastic-growth factor (BFGF), and hepatocyte-growth factor. _In vitro_, lenalidomide inhibits cell adhesion molecules such as ICAM-1, LFA-1, β2 and β3 integrins, as well as gap-junction function, thereby preventing metastasis of malignant cells. |
| Pharmacodynamics | In hematological malignancies, the immune system is deregulated in the form of altered cytokine networks in the tumour microenvironment, defective T cell regulation of host-tumour immune interactions, and diminished NK cell activity. Lenalidomide is an immunomodulatory agent with antineoplastic, antiangiogenic, and anti-inflammatory properties. Lenalidomide exerts direct cytotoxicity by increasing apoptosis and inhibiting the proliferation of hematopoietic malignant cells. It delays tumour growth in nonclinical hematopoietic tumour models _in vivo_, including multiple myeloma. Lenalidomide also works to limit the invasion or metastasis of tumour cells and inhibits angiogenesis. Lenalidomide also mediates indirect antitumour effects via its immunomodulatory actions: it inhibits the production of pro-inflammatory cytokines, which are implicated in various hematologic malignancies. Lenalidomide enhances the host immunity by stimulating T cell proliferation and enhancing the activity of natural killer (NK) cells.[A713, A228703, A228708] Lenalidomide is about 100–1000 times more potent in stimulating T cell proliferation than [thalidomide]. _In vitro_, it enhances antibody-dependent cell-mediated cytotoxicity (ADCC), which is even more pronounced when used in combination with rituximab. Due to its anti-inflammatory properties, lenalidomide has been investigated in the context of inflammatory and autoimmune diseases, such as amyotrophic lateral sclerosis. |
Targets
| Target | Organism | Actions |
|---|---|---|
| Protein cereblon | Humans | inhibitor |
| Tumor necrosis factor ligand superfamily member 11 | Humans | inhibitor |
| Cadherin-5 | Humans | antagonist |
ADME / PK
| Absorption | Following oral administration, lenalidomide is rapidly absorbed with high bioavailability. It has a T<sub>max</sub> ranging from 0.5 to six hours. Lenalidomide exhibits a linear pharmacokinetic profile, with its AUC and C<sub>max</sub> increasing proportionally with dose. Multiple dosing does not result in drug accumulation. In healthy male subjects, the C<sub>max</sub> was 413 ± 77 ng/ml and the AUC<sub>infinity</sub> was 1319 ± 162 h x ng/ml. |
|---|---|
| Half-life | In healthy subjects, the mean half-life of lenalidomide is three hours in the clinically relevant dose range (5–50 mg). Half-life can range from three to five hours in patients with multiple myeloma, myelodysplastic syndromes, or mantle cell lymphoma. |
| Protein binding | _In vitro_, about 30% of lenalidomide was bound to plasma proteins. |
| Metabolism | Lenalidomide is not subject to extensive hepatic metabolism involving CYP enzymes and metabolism contributes to a very minor extent to the clearance of lenalidomide in humans. Lenalidomide undergoes hydrolysis in human plasma to form 5-hydroxy-lenalidomide and N-acetyl-lenalidomide. Unchanged lenalidomide is the predominant circulating drug form, with metabolites accounting for less than five percent of the parent drug levels in the circulation. |
| Route of elimination | Lenalidomide is eliminated predominantly via urinary excretion in the unchanged form. Following oral administration of 25 mg of radiolabeled lenalidomide in healthy subjects, about 90% of the dose (4.59% as metabolites) was eliminated in urine and 4% of the dose (1.83% as metabolites) was eliminated in feces within ten days post-dose. Approximately 85% of the dose was excreted as lenalidomide in the urine within 24 hours. |
| Volume of distribution | In healthy male subjects, the apparent volume of distribution was 75.8 ± 7.3 L. |
| Clearance | The renal clearance of lenalidomide exceeds the glomerular filtration rate. In healthy male subjects, the oral clearance was 318 ± 41 mL/min. |
Formulation & handling
- Lenalidomide is a small molecule administered exclusively via oral capsules in multiple dosages.
- It is not a peptide or biologic and has modest lipophilicity (LogP -0.71) indicating moderate solubility characteristics.
- The API can be taken with or without food, though high-fat meals may reduce absorption without significant clinical impact.
Regulatory status
| Lifecycle | The API's patent protection in Canada and the United States has expired or will expire between 2014 and 2023, indicating that the product is in a mature market phase in Canada and the US, while it continues to be marketed in the EU. |
|---|
| Markets | Canada, US, EU |
|---|
Supply Chain
| Supply chain summary | The manufacturing landscape for lenalidomide involves primarily two originator companies responsible for both production and packaging, with packaging also carried out by third-party providers. The branded product has a strong presence in North America and the European Union markets. Multiple patents have expired or are near expiration in Canada and the United States, indicating the potential for existing or forthcoming generic competition. |
|---|
Safety
| Toxicity | The lowest lethal dose (LDLo) in rats is >2000 mg/kg following oral administration and >40 mg/kg following intravenous administration. The oral Lowest published toxic dose (TDLo) in humans is 9 mg/kg/4W (intermittent). There is limited clinical experience in managing lenalidomide overdose. In single-dose studies, healthy subjects have been exposed to doses up to 400 mg. In clinical trials, the dose-limiting toxicity was neutropenia and thrombocytopenia. Toxicities associated with lenalidomide, some leading to fatality, include embryo-fetal toxicity, neutropenia, thrombocytopenia, venous (deep vein thrombosis and pulmonary embolism) and arterial thromboembolic events (myocardial infarction and stroke), serious adverse cardiovascular reactions, second primary malignancies, hepatotoxicity, severe cutaneous reactions, tumour lysis syndrome, tumour flare reaction, hypothyroidism, and hyperthyroidism. |
|---|
- Lenalidomide exhibits dose-dependent hematologic toxicity, including neutropenia and thrombocytopenia, which may be dose-limiting
- Overdose management experience is limited
- Lethal dose thresholds vary by administration route (oral LDLo ›2000 mg/kg in rats
Lenalidomide is a type of Immunomodulators
Immunomodulators, a category of pharmaceutical active pharmaceutical ingredients (APIs), are substances that help regulate and modify the immune response of an individual. These compounds play a crucial role in treating various immune-related disorders and diseases. Immunomodulators work by either enhancing or suppressing the immune system, depending on the specific condition being treated.
Immunomodulators are used in the treatment of autoimmune disorders, such as rheumatoid arthritis, multiple sclerosis, and psoriasis. By suppressing the immune system, these APIs help reduce the overactive immune response associated with these conditions, thereby alleviating symptoms and preventing further damage to the body's tissues.
On the other hand, immunomodulators are also employed to boost the immune system in cases of immunodeficiency disorders. These APIs stimulate the immune response, enabling the body to better fight off infections and diseases. Additionally, immunomodulators are utilized in the prevention and treatment of organ transplant rejection, where they help modulate the immune system to accept the transplanted organ.
The development and production of immunomodulators require rigorous testing and quality control to ensure their safety and efficacy. Pharmaceutical companies carefully formulate these APIs into various dosage forms, including tablets, capsules, injections, and topical preparations, to cater to different patient needs.
In summary, immunomodulators form a vital category of pharmaceutical APIs that regulate and modify the immune system. With their ability to modulate immune responses, these compounds contribute significantly to the management and treatment of various immune-related disorders and diseases, improving the quality of life for many patients.
Lenalidomide API manufacturers & distributors
Compare qualified Lenalidomide API suppliers worldwide. We currently have 20 companies offering Lenalidomide 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 |
|---|---|---|---|---|---|
| Arshine Pharmaceutical Co... | Distributor | China | China | BSE/TSE, CEP, CoA, FDA, GMP, MSDS, USDMF | 176 products |
| Changzhou Pharma | Producer | China | China | CoA, USDMF | 9 products |
| Chongqing Jooe Co., Ltd. | Producer | China | China | CoA, FDA, GMP, MSDS | 10 products |
| Cipla | Producer | India | India | CoA, GMP, USDMF, WC | 164 products |
| Dr. Reddy's | Producer | India | India | BSE/TSE, CoA, EDMF/ASMF, FDA, GMP, MSDS, USDMF, WC | 170 products |
| Global Pharma Tek | Distributor | India | India | BSE/TSE, CoA, FDA, GMP, ISO9001, MSDS | 484 products |
| Hetero Labs | Producer | India | India | CoA, USDMF | 90 products |
| Laurus Labs | Producer | India | India | CoA, GMP, WC | 50 products |
| MSN Labs. | Producer | India | India | CoA, GMP, USDMF, WC | 119 products |
| Mylan | Producer | India | India | CoA, GMP, USDMF, WC | 201 products |
| Qilu Antibiotics | Producer | China | China | CoA, WC | 33 products |
| Reliance Life Sciences | Producer | India | India | CoA, USDMF, WC | 11 products |
| Rochem International, Inc... | Distributor | United States | United States | BSE/TSE, CoA, GMP, ISO9001, MSDS | 144 products |
| Shandong Boyuan | Producer | China | China | BSE/TSE, CoA, MSDS | 55 products |
| Shaoxing Hantai Pharma | Distributor | China | China | CoA | 162 products |
| Shilpa Medicare Ltd | Producer | India | India | BSE/TSE, CoA, GMP, ISO9001, MSDS, USDMF, WC | 54 products |
| Shivalik Rasayan Ltd. | Producer | India | India | CoA, GMP, USDMF, WC, WHO-GMP | 13 products |
| Sinoway industrial Co.,Lt... | Distributor | China | China | CEP, CoA, GMP, ISO9001, MSDS, USDMF | 757 products |
| Sun Pharma | Producer | India | India | CoA, GMP, USDMF, WC | 219 products |
| Yangtze River Pharmaceuti... | Producer | China | China | CoA, FDA, GMP, ISO14001 | 34 products |
When sending a request, specify which Lenalidomide 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 Lenalidomide 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.
