EFALIZUMABUM
- CAS No.
- 214745-43-4
- Chemical Name:
- EFALIZUMABUM
- Synonyms
- EFALIZUMABUM;Hu1124|||HU 1124;Efalizumab (anti-ITGAL);Research Grade Efalizumab(DHD41001)
- CBNumber:
- CB72631887
- Molecular Formula:
- Molecular Weight:
- 0
- MDL Number:
- MOL File:
- Mol file
form | Liquid |
---|---|
color | Colorless to light yellow |
FDA UNII | XX2MN88N5D |
EFALIZUMABUM Chemical Properties,Uses,Production
Description
Efalizumab, a humanized monoclonal antibody marketed for the treatment of psoriasis, is a full-length IgG1 antibody developed through a murine anti-human CD11a mAb. It is produced in a Chinese hamster ovary mammalian cell expression system in a nutrient medium containing the antibiotic gentamicin. Psoriasis is a disease mediated through inflammatory cells (primarily T-cells expressing CD4 or CD8 markers) and keratinocytes. CD11a is the alpha-chain LFA-1 (leukocyte function associate antigen; integrin family). It is expressed on the surface of Tlymphocytes and it binds to the intercellular cell adhesion molecules (ICAM-1, -2 and -3) on endothelial cells, monocytes, keratinocytes, fibroblasts, and activated lymphocytes. By blocking LFA-1 binding the ability of T cells to adhere, migrate and be activated is blunted. Studies in chimpanzee and murine animal models demonstrated that efalizumab down regulates the expression of LFA-1 on lymphocytes, prevents contact dermatitis to 2,4-dinitrofluorobenzene, increases skin and heart transplant survival. In the collagen-induced arthritis model it delays onset and decreases the severity of the arthritic condition. In a study of 498 patients, efalizumab treatment of 1 or 2 mg/kg/wk for 12 weeks provided, respectively, a 39 or 27% Psoriasis Area and Severity Score (PASI) improvement of ≥75%. By comparison, placebo provided a 2% improvement. It was further demonstrated that a second 12-week course could provide additional improvement. As dose increases, clearance decreases (dose 0.1 mg/kg: 322 ml/day/kg; dose 10 mg/kg: 6.6 mL/day/kg) with data suggesting saturation of clearance above 10 mg/mL. A pharmacokinetic model positively correlates number of circulating cells expressing CD11a with relative clearance. This blockade decreases the CD11a expressed on circulating lymphocytes to about 25% of their baseline levels in patients with plaque psoriasis. Efalizumab is formulated as a once-weekly subcutaneous injectable, dosed at 0.7 to 1 mg/kg/week. Although mild adverse events were noted such as headache, pain chills, nausea, and fever, these events generally decreased after one or two doses. The overall rate of infections was only 3% higher than the placebo-arm and no depletion of T-cells was noted.
Originator
XOMA (US)
Uses
Treatment of transplant rejections; antipsoriatic (immunomodulator monoclonal antibody which decreases the activation, migration, and adhesion of T-cells). hu1124; anti-CD11a.
brand name
Raptiva
EFALIZUMABUM Preparation Products And Raw materials
Raw materials
Preparation Products
EFALIZUMABUM Suppliers
Supplier | Tel | Country | ProdList | Advantage | |
---|---|---|---|---|---|
Aladdin Scientific | +1-+1(833)-552-7181 | sales@aladdinsci.com | United States | 57511 | 58 |
Wuhan Chemstan Biotechnology Co., Ltd. | 027-65317797 15926423062 | 422450190@qq.com | China | 10351 | 58 |
ShangHai Biochempartner Co.,Ltd | 17754423994 17754423994 | 2853530910@QQ.com | China | 8014 | 62 |
Guangzhou Hongyuan Chemical Co.,Ltd | 15817493340 | 981810490@qq.com | China | 1565 | 58 |
TargetMol Chemicals Inc. | 4008200310 | marketing@tsbiochem.com | China | 24647 | 58 |
Biolab Reagents | 027-65279366 18162686757 | products@biolabreagent.com | China | 9818 | 58 |
Wuhan Jingkangen Biomedical Technology Co., Ltd | 13720134139 13720134139 | orders@jknbiochem.com | China | 5782 | 58 |
Shanghai Yifei Biotechnology Co. , Ltd. | 021-65675885 18964387627 | customer_service@efebio.com | China | 11975 | 58 |
Shanghai Aladdin Biochemical Technology Co.,Ltd. | +86-18521732826 | market@aladdin-e.com | China | 48465 | 58 |
Changsha Fuzhen Biotechnology Co.,LTD | 13823398779 18670069958 | 313359644@qq.com | China | 3263 | 58 |