Bevacizumab Monoclonal Antibody

English name：Bevacizumab monoclonal antibody

CAS number：216974-75-3

molecular formula：C6638H10160N1720O2108S44

EINECS number：200-160-3

Related:Drug substance; mab 5; drug substance and intermediates; chemical reagent

Constitutional formula:

Morphological ：liquid

Color：Colourless to light yellow

condition of storage： Store at -80°C

Solubility: dissolved in dimethyl sulfoxide

Summary

Avastin, developed by Roche and approved by the US Food and Drug Administration (FDA) in 2004 and marketed in the US in March, is currently the first monoclonal antibody drug approved to inhibit vascular growth. By inhibiting vascular endothelial growth factor (VascuChemicalbooklaren-dothelialgrowthfactor, VE GF), tumor tissue is unable to obtain the required blood, oxygen and other nutrients and kills tumor cells, thus achieving anti-cancer efficacy. It can be used in most tumors and more commonly used for the treatment of metastatic colorectal cancer and lung cancer.

Pharmacological action

As an anti-vascular proliferation drug, it is an IgG 1 monoclonal antibody targeting vascular endothelial growth factor (VE GF), which competitively inhibits the binding of vascular endothelial cell surface receptors to VE GF, thus exerting an anti-vascular proliferation effect.

mechanism of action

Bevacizumab achieves anti-tumor therapeutic effect by blocking vascular endothelial growth factor VE GF, inhibiting tumor angiogenesis, cutting off blood supply to the tumor area, and inhibiting tumor growth and metastasis, and Chemicalbook induces tumor cell apoptosis. Moreover, bevacizumab is highly specific, and blocking the VE GF pathway usually does not interfere with other targets.

Apply

1.Used in the clinical treatment of tumors, such as in the treatment of psoriasis.

2.For the first-line treatment of patients with advanced colorectal cancer

3.For colon cancer and can also be used for breast cancer and lung Chemicalbook cancer. Overview, pharmacological effects, indications, adverse reactions, etc.

Untoward effect

The most serious adverse reactions were gastrointestinal perforation, wound complications, bleeding, hypertensive crisis, nephrotic syndrome, and congestive heart failure. The most common serious adverse reactions were weakness, pain, hypertension, diarrhea, and Chemicalbook cell reduction. The most common adverse reactions are: weakness, pain, abdominal pain, headache, high blood pressure, diarrhea, nausea, vomiting, decreased appetite, stomatitis, constipation, upper respiratory tract infection, epistaxis, dyspnea, exfoliative dermatitis, and proteinuria.

bioactivity

Bevacizumab (anti-VE GF, Avastin) is a humanized anti-VE GF monoclonal antibody, Chemicalbook, which is an inhibitor of VE GF. Can bind and neutralizing with human-derived VE GF-A isoforms (and biologically active proteolytic fragments).MW:149KD.

Target spot

Target Value

VEGFR2

()

VEGF-A

()

VEGF

()

In vitro study

Gly 88 of human VE GF is essentially required for bevacizumab binding and also guarantees species specificity of bevacizumab binding with rat and mouse VE GF is a serine Chemicalbook acid residue at this corresponding position.bevacizumab May bind to and neutralize the all-derived VE GF-A isoform (and bioactive proteolytic fragments) without neutralizing other VE GF gene family members, such as VE GF-B or VE GF-C.

In vivo research

In humans, the terminal half-life of bevacizumab is 17 – 21 days. In nude mice, Bevacizumab inhibited the growth of human tumor cell lines with maximum inhibition at doses of 1-2mg / kg (twice a week). The dose required for half-maximal inhibition was 0.1-0.5mg/kg. A safety assessment study of bevacizumab in Macacafascicularis (cynomolgusmonkey), with bevacizumab administration for 4-13 weeks, young adults: dose-dependent increase of hypertrophic chondrocytes Chemicalbook, inhibition of vascular invasion in the growth zone. Administration of long-term bevacizumab inhibited vascular growth in the female system, weight loss in the ovary and uterus, and loss of the corpus luteum. The changes in the growth plate and ovary were reversible and could recover gradually after cessation of treatment. Moreover, no other administration-related side effects were observed at drug concentrations up to 50mg / kg. After subcutaneous injection, the bioavailability of rhuMAbVEGF (bevacizumab) was 69% in rats, compared with 100% in mice and cynomolgus monkeys. Bevacizumab binds to primate VE GF and to rabbit VE GF with low affinity, but not to rat and mouse VE GF.

Security information

Toxic substances data: 216974-75-3 (Hazardous Substances Data)

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