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| Primary information |
|---|
| ID | 10731 |
| Therapeutic ID | Th1167 |
| Protein Name | Atezolizumab |
| Sequence | >Th1167_Atezolizumab
EVQLVESGGGLVQPGGSLRLSCAASGFTFSDSWIHWVRQAPGKGLEWVAWISPYGGSTYYADSVKGRFTISADTSKNTAYLQMNSLRAEDTAVYYCARRHWPGGFDYWGQGTLVTVSSASTKGPSVFPLAPSSKSTSGGTAALGCLVKDYFPEPVTVSWNSGALTSGVHTFPAVLQSSGLYSLSSVVTVPSSSLGTQTYICNVNHKPSNTKVDKKVEPKSCDKTHTCPPCPAPELLGGPSVFLFPPKPKDTLMISRTPEVTCVVVDVSHEDPEVKFNWYVDGVEVHNAKTKPREEQYASTYRVVSVLTVLHQDWLNGKEYKCKVSNKALPAPIEKTISKAKGQPREPQVYTLPPSREEMTKNQVSLTCLVKGFYPSDIAVEWESNGQPENNYKTTPPVLDSDGSFFLYSKLTVDKSRWQQGNVFSCSVMHEALHNHYTQKSLSLSPGK
|
| Molecular Weight | 145000 |
| Chemical Formula | NA |
| Isoelectric Point | 6.6-7.2 |
| Hydrophobicity | NA |
| Melting point | 78 °C |
| Half-life | Terminal half-life was 27 days |
| Description | Atezolizumab is an Fc-engineered, humanized, monoclonal antibody that binds to PD-L1 and blocks interactions with the PD-1 and B7.1 receptors. Atezolizumab is a non-glycosylated IgG1 kappa immunoglobulin that has a calculated molecular mass of 145 kDa. Atezolizumab was approved in the US in May, 2016 under the brand name Tecentriq. |
| Indication/Disease | For the treatment of patients with locally advanced or metastatic urothelial carcinoma who: 1) have disease progression during or following platinum-containing chemotherapy; and 2) have disease progression within 12 months of neoadjuvant or adjuvant treatment with platinum-containing chemotherapy. |
| Pharmacodynamics | Atezolizumab is a monoclonal antibody that binds to PD-L1 and blocks its interactions with both PD-1 and B7.1 receptors. This releases the PD-L1/PD-1 mediated inhibition of the immune response, including activation of the anti-tumor immune response without inducing antibodydependent cellular cytotoxicity. In syngeneic mouse tumor models, blocking PD-L1 activity resulted in decreased tumor growth. |
| Mechanism of Action | PD-L1 may be expressed on tumor cells and/or tumor-infiltrating immune cells and can contribute to the inhibition of the anti-tumor immune response in the tumor microenvironment. Binding of PD-L1 to the PD-1 and B7.1 receptors found on T cells and antigen presenting cells suppresses cytotoxic T-cell activity, T-cell proliferation and cytokine production. |
| Toxicity | Most common adverse reactions (= 20% of patients) included: fatigue, decreased appetite, nausea, urinary tract infection, pyrexia, and constipation. Overdose data for atezolizumab is scarce[A181241] but the most common adverse reactions are fatigue, nausea, cough, dyspnea, decreased appetite, alopecia, constipation, diarrhea, peripheral neuropathies, anemia, headache, neutropenia, and vomiting.[L7489] |
| Metabolism | Monoclonal antibodies are broken down into smaller polypeptides and amino acids.[A31470] |
| Absorption | Pharmacokinetic analysis was performed in patients with metastatic urothelial carcinoma.[A181223] In these patients, the AUC was 2.19-2.73day |
| The volume of distribution of atezolizumab is 6.91L.[A18492,A181223] |
| Clearance | The clearance of atezolizumab is 0.200L/day.[A18492,A181223] |
| Categories | NA |
| Patents Number | NA |
| Date of Issue | NA |
| Date of Expiry | NA |
| Drug Interaction | NA |
| Target | Programmed cell death 1 ligand 1 |
| Brand Name | Tecentriq |
| Company | NA |
| Brand Description | NA |
| Prescribed For | It is indicated for the treatment of patients with locally advanced or metastatic urothelial carcinoma who: Have disease progression during or following platinum-containing chemotherapy. Have disease progression within 12 months of neoadjuvant or adjuvant treatment with platinum-containing chemotherapy |
| Chemical Name | NA |
| Formulation | NA |
| Physical Appearance | NA |
| Route of Administration | NA |
| Recommended Dosage | The recommended dose of TECENTRIQ is 1200 mg administered as an intravenous infusion over 60 minutes every 3 weeks until disease progression or unacceptable toxicity. If the first infusion is tolerated, all subsequent infusions may be delivered over 30 minutes. Do not administer TECENTRIQ as an intravenous push or bolus. |
| Contraindication | NA |
| Side Effects | Immune-Related Pneumonitis; Immune-Related Hepatitis; Immune-Related Colitis; Immune-Related Endocrinopathies; Other Immune-Related Adverse Reactions; Infection; Infusion-Related Reactions. |
| Useful Link 1 | Link |
| Useful Link 2 | NA |
| Remarks | NA |