Lenalidomide Basic information
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Product Name: |
Lenalidomide |
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Synonyms: |
enalidomide;Lenalidomid;Revlimid;3-(4-amino-1-oxoisoindolin-2-yl)piperidine-2,6-dione,Lenalidomide;LenalidoMide(CC-5013,RevliMid);Lenalidomide ,98%;3-(4-amino-1-oxoisoindolin-2-yl)piperidine-2,6-dione;(3S)-3-(4-Amino-1-oxo-1,3-dihydro-2H-isoindol-2-yl)piperidine-2,6-dione |
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CAS: |
191732-72-6 |
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MF: |
C13H13N3O3 |
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MW: |
259.261 |
Lenalidomide Chemical Properties
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Melting point |
265-268°C |
| Boiling point | 614.0±55.0 °C(Predicted) |
| density | 1.460±0.06 g/cm3(Predicted) |
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storage temp. |
2-8℃ |
| solubility | Soluble in DMSO (up to 30 mg/ml) |
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form |
Solid |
| pka | 10.75±0.40(Predicted) |
| color | White |
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Stability |
Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months. |
Lenalidomide Usage And Synthesis
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Uses |
Lenalidomide (Revlimid, CC-5013) is a TNF-α secretion inhibitor with IC50 of 13 nM. Lenalidomide is a thalidomide analog known to have immunomodulatory properties. Lenalidomide inhibits TNF-alpha production, stimulates T cells, reduces serum levels of the cytokines vascular endothelial growth factor (VEGF) and basic fibroblast growth factor (bFGF), and inhibits angiogenesis. This agent also promotes G1 cell cycle arrest and apoptosis of malignant cells. It is used in the therapy of multiple myeloma. |
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Description |
Lenalidomide is a kind of antitumor drugs that developed by American biological pharmaceutical companies. Its chemical structure is similar with thalidomide. It differing in the presence of an amino moiety in the 4-position and removal of one of the carbonyls of the phthaloyl ring. This derivative evolved from a structural-based effort to eliminate the adverse effects (somnolence, neuropathy, and teratogenicity) of thalidomide while maintaining or enhancing the appealing attributes. It has many functions such as anti-tumor, immune regulation and anti-angiogenesis. It can inhibit the secretion of inflammatory cytokines, and increase the secretion of peripheral blood mononuclear anti-inflammatory cytokines. Vitro tests show that lenalidomide can inhibit the hyperplasia of some cell lines such as namalwa cell. It can inhibit the growth of patients' multiple myeloma cells and MM1S cell. In addition, lenalidomide also can inhibit the expression of oxidase-2 (COX-2), but it has no effect on COX-1. Two multicenter randomized double-blind placebo-controlled clinical studies evaluate the safety and curative effect of lenalidomide that is used for multiple myeloma. The primary efficacy end point of the studies is time to progression (TTP). The interim analysis shows that TTP of the combination group is significantly superior to dexamethasone group. Recent clinical research results show that lenalidomide not only has curative effect on treating MDS and MM, but also on treating myeloma, leukemia, metastatic renal cell carcinoma, solid tumor, idiopathic generalized amyloidosis and systemic bone marrow fibrosis disease with marrow unripe. |
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Chemical Properties |
Yellow Solid |
Dosage
It must be started and provided under the supervision of a doctor with experience in the treatment of multiple myeloma.
The recommended starting dose of this product is 25mg. On the 1st to 21st days of each repeated 28-day cycle, the product is orally taken 25 mg daily until disease progression. The recommended dose of dexamethasone is 40 mg dexamethasone taken orally on days 1, 8, 15, and 22 of each 28-day treatment cycle. The prescribing doctor should carefully select the initial dose and subsequent dose adjustment of this product according to the patient's renal function, and should select the initial dose and subsequent dose adjustment of dexamethasone according to the patient's age.
Adverse reactions
The most common adverse reactions of lenalidomide are thrombocytopenia (21.5%) and neutropenia (42.2%). Other common adverse reactions include diarrhea, itching, rash, fatigue, constipation, nausea, nasopharyngitis, arthralgia, fever, back pain, peripheral edema, cough, dizziness, headache, muscle cramps, difficulty breathing and pharyngitis.
Every time a physician prescribes it to a patient, he should provide guidance to the patient. The physician or pharmacist should take this opportunity to explain the possible risks of lenalidomide to the patient. It is best for patients who are going to take medicine to take two different effective contraceptive measures at the same time. Female patients planning to take lenalidomide should sign an informed consent form under the guidance of a doctor to show that they already know the importance of contraception when taking lenalidomide. In addition, all female patients with a possibility of pregnancy need to undergo two pregnancy tests before medication (one is scheduled for 10 to 14 days before administration, and the other is scheduled within 24 hours before administration). Only two pregnancy tests are performed Only those with negative results can formally take lenalidomide.
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