Identification
- Summary
Atezolizumab is a monoclonal antibody used to treat advanced or metastatic urothelial carcinoma with disease progression during or up to 12 months after platinum-containing chemotherapy.
- Brand Names
- Tecentriq
- Generic Name
- Atezolizumab
- DrugBank Accession Number
- DB11595
- Background
Atezolizumab is a humanized monoclonal antibody used to prevent the interaction of PD-L1 and PD-1, removing inhibition of immune responses seen in some cancers.2,7 This medication is reserved for patients whose tumors express PD-L1, cannot receive platinum based chemotherapy, or whose tumors do not respond to platinum based chemotherapy.7 Atezolizumab was granted FDA approval on 18 October 2016.7
- Type
- Biotech
- Groups
- Approved, Investigational
- Biologic Classification
- Protein Based Therapies
Monoclonal antibody (mAb) - Protein Chemical Formula
- Not Available
- Protein Average Weight
- 145000.0 Da
- Sequences
>Heavy Chain Sequence EVQLVESGGGLVQPGGSLRLSCAASGFTFSDSWIHWVRQAPGKGLEWVAWISPYGGSTYY ADSVKGRFTISADTSKNTAYLQMNSLRAEDTAVYYCARRHWPGGFDYWGQGTLVTVSSAS TKGPSVFPLAPSSKSTSGGTAALGCLVKDYFPEPVTVSWNSGALTSGVHTFPAVLQSSGL YSLSSVVTVPSSSLGTQTYICNVNHKPSNTKVDKKVEPKSCDKTHTCPPCPAPELLGGPS VFLFPPKPKDTLMISRTPEVTCVVVDVSHEDPEVKFNWYVDGVEVHNAKTKPREEQYAST YRVVSVLTVLHQDWLNGKEYKCKVSNKALPAPIEKTISKAKGQPREPQVYTLPPSREEMT KNQVSLTCLVKGFYPSDIAVEWESNGQPENNYKTTPPVLDSDGSFFLYSKLTVDKSRWQQ GNVFSCSVMHEALHNHYTQKSLSLSPGK
>Light Chain Sequence DIQMTQSPSSLSASVGDRVTITCRASQDVSTAVAWYQQKPGKAPKLLIYSASFLYSGVPS RFSGSGSGTDFTLTISSLQPEDFATYYCQQYLYHPATFGQGTKVEIKRTVAAPSVFIFPP SDEQLKSGTASVVCLLNNFYPREAKVQWKVDNALQSGNSQESVTEQDSKDSTYSLSSTLT LSKADYEKHKVYACEVTHQGLSSPVTKSFNRGEC
Download FASTA Format- Synonyms
- Atezolizumab
- External IDs
- MPDL 3280A
- MPDL-3280A
- MPDL3280A
- RG-7446
- RG7446
Pharmacology
- Indication
Atezolizumab is indicated to treat locally or advanced metastatic urothelial carcinoma in patients ineligible for cicplatin-containing chemotherapy with tumors expressing PD-L1, in patients ineligible for cisplatin-containing chemotherapy irrespective of PD-L1, have disease progression following platinum containing chemotherapy, or have disease progression within 12 months of neoadjuvant or adjuvant chemotherapy.7
Atezolizumab is also indicated first line for non small cell lung cancer in combination with bevacizumab, paclitaxel, and carboplatin with no EGFR or ALK genomic abnormalities.7 It can be used in patients with disease progression during or after platinum containing chemotherapy even if they have EGFR and ALK abnormalities.7
Atezolizumab is indicated in combination with paclitaxel protein-bound to treat locally advanced or metastatic triple negative breast cancer expressing PD-L1.7
Finally, atezolizumab is indicated in combination with carboplatin and etoposide as first line treatment for extensive stage small cell lung cancer.7
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- Contraindications & Blackbox Warnings
Avoid life-threatening adverse drug eventsImprove clinical decision support with information on contraindications & blackbox warnings, population restrictions, harmful risks, & more.Avoid life-threatening adverse drug events & improve clinical decision support.- Pharmacodynamics
Atezolizumab is a humanized monoclonal antibody used to prevent the interaction of PD-L1 and PD-1, removing inhibition of immune responses seen in some cancers.2,7 This drug has a long duration of action as it is usually given every 3-4 weeks.7 Atezolizumab should not be used in patients with immune mediated penumonitis, hepatitis, colitis, and some endocrinopathies.7
- Mechanism of action
Atezolizumab is a humanized IgG antibody that binds PD-L1, preventing its interaction with PD-1 and B7-1.2 Preventing the interaction of PD-L1 and PD-1 removes inhibition of immune responses such as the anti-tumor immune response but not antibody dependent cellular cytotoxicity.7
Target Actions Organism AProgrammed cell death 1 ligand 1 inhibitorantibodyHumans - Absorption
Pharmacokinetic analysis was performed in patients with metastatic urothelial carcinoma.3 In these patients, the AUC was 2.19-2.73day*µg/mL/mg, the Cmax was 0.27-0.35µg/mL/mg, and the Cmin was 0.004-0.008µg/mL/mg.3
- Volume of distribution
- Protein binding
Monoclonal antibodies are not expected to bind to proteins in plasma they are not designed to target.
- Metabolism
Monoclonal antibodies are broken down into smaller polypeptides and amino acids.4
- Route of elimination
Atezolizumab is not renally excreted.5
- Half-life
- Clearance
- Adverse Effects
Improve decision support & research outcomesWith structured adverse effects data, including: blackbox warnings, adverse reactions, warning & precautions, & incidence rates.Improve decision support & research outcomes with our structured adverse effects data.- Toxicity
Most common adverse reactions (≥ 20% of patients) included: fatigue, decreased appetite, nausea, urinary tract infection, pyrexia, and constipation.
Overdose data for atezolizumab is scarce6 but the most common adverse reactions are fatigue, nausea, cough, dyspnea, decreased appetite, alopecia, constipation, diarrhea, peripheral neuropathies, anemia, headache, neutropenia, and vomiting.7
- Pathways
- Not Available
- Pharmacogenomic Effects/ADRs
- Not Available
Interactions
- Drug Interactions
- This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
Drug Interaction Integrate drug-drug
interactions in your softwareAbciximab The risk or severity of adverse effects can be increased when Abciximab is combined with Atezolizumab. Adalimumab The risk or severity of adverse effects can be increased when Adalimumab is combined with Atezolizumab. Aducanumab The risk or severity of adverse effects can be increased when Atezolizumab is combined with Aducanumab. Alemtuzumab The risk or severity of adverse effects can be increased when Alemtuzumab is combined with Atezolizumab. Alirocumab The risk or severity of adverse effects can be increased when Alirocumab is combined with Atezolizumab. Amivantamab The risk or severity of adverse effects can be increased when Atezolizumab is combined with Amivantamab. Anifrolumab The risk or severity of adverse effects can be increased when Atezolizumab is combined with Anifrolumab. Ansuvimab The risk or severity of adverse effects can be increased when Atezolizumab is combined with Ansuvimab. Anthrax immune globulin human The risk or severity of adverse effects can be increased when Anthrax immune globulin human is combined with Atezolizumab. Antilymphocyte immunoglobulin (horse) The risk or severity of adverse effects can be increased when Antilymphocyte immunoglobulin (horse) is combined with Atezolizumab. 
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- No interactions found.
Products
Drug product information from 10+ global regionsOur datasets provide approved product information including:dosage, form, labeller, route of administration, and marketing period.Access drug product information from over 10 global regions.- Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Tecentriq Solution 1200 mg / 20 mL Intravenous Hoffmann La Roche 2017-05-02 Not applicable Canada 
Tecentriq Injection, solution, concentrate 1200 mg Intravenous Roche Registration Gmb H 2020-12-16 Not applicable EU 
Tecentriq Injection, solution 840 mg/14mL Intravenous Genentech, Inc. 2019-03-08 Not applicable US 
Tecentriq Solution 840 mg / 14 mL Intravenous Hoffmann La Roche 2019-10-16 Not applicable Canada Tecentriq Injection, solution, concentrate 840 mg Intravenous Roche Registration Gmb H 2020-12-16 Not applicable EU Tecentriq Injection, solution 1200 mg/20mL Intravenous Genentech, Inc. 2016-05-18 Not applicable US
Categories
- ATC Codes
- L01XC32 — Atezolizumab
- Drug Categories
- Amino Acids, Peptides, and Proteins
- Antibodies
- Antibodies, Monoclonal
- Antibodies, Monoclonal, Humanized
- Antineoplastic Agents
- Antineoplastic and Immunomodulating Agents
- Blood Proteins
- Cancer immunotherapy
- Globulins
- Immune Checkpoint Inhibitors
- Immunoglobulins
- Immunoproteins
- Immunotherapy
- Narrow Therapeutic Index Drugs
- Programmed Death Receptor-1 Blocking Antibody
- Programmed Death Receptor-1-directed Antibody Interactions
- Proteins
- Serum Globulins
- Chemical TaxonomyProvided by Classyfire
- Description
- Not Available
- Kingdom
- Organic Compounds
- Super Class
- Organic Acids
- Class
- Carboxylic Acids and Derivatives
- Sub Class
- Amino Acids, Peptides, and Analogues
- Direct Parent
- Peptides
- Alternative Parents
- Not Available
- Substituents
- Not Available
- Molecular Framework
- Not Available
- External Descriptors
- Not Available
- Affected organisms
- Not Available
Chemical Identifiers
- UNII
- 52CMI0WC3Y
- CAS number
- 1380723-44-3
References
- General References
- Markham A: Atezolizumab: First Global Approval. Drugs. 2016 Aug;76(12):1227-32. doi: 10.1007/s40265-016-0618-8. [Article]
- Rosenberg JE, Hoffman-Censits J, Powles T, van der Heijden MS, Balar AV, Necchi A, Dawson N, O'Donnell PH, Balmanoukian A, Loriot Y, Srinivas S, Retz MM, Grivas P, Joseph RW, Galsky MD, Fleming MT, Petrylak DP, Perez-Gracia JL, Burris HA, Castellano D, Canil C, Bellmunt J, Bajorin D, Nickles D, Bourgon R, Frampton GM, Cui N, Mariathasan S, Abidoye O, Fine GD, Dreicer R: Atezolizumab in patients with locally advanced and metastatic urothelial carcinoma who have progressed following treatment with platinum-based chemotherapy: a single-arm, multicentre, phase 2 trial. Lancet. 2016 May 7;387(10031):1909-20. doi: 10.1016/S0140-6736(16)00561-4. Epub 2016 Mar 4. [Article]
- Stroh M, Winter H, Marchand M, Claret L, Eppler S, Ruppel J, Abidoye O, Teng SL, Lin WT, Dayog S, Bruno R, Jin J, Girish S: Clinical Pharmacokinetics and Pharmacodynamics of Atezolizumab in Metastatic Urothelial Carcinoma. Clin Pharmacol Ther. 2017 Aug;102(2):305-312. doi: 10.1002/cpt.587. Epub 2017 Jun 9. [Article]
- Tabrizi MA, Tseng CM, Roskos LK: Elimination mechanisms of therapeutic monoclonal antibodies. Drug Discov Today. 2006 Jan;11(1-2):81-8. doi: 10.1016/S1359-6446(05)03638-X. [Article]
- Mann, Janelle: Atezolizumab (Tecentriq®) Oncology Times. 2017 Feb 25;39(4):31. [Article]
- Raschi E, Mazzarella A, Antonazzo IC, Bendinelli N, Forcesi E, Tuccori M, Moretti U, Poluzzi E, De Ponti F: Toxicities with Immune Checkpoint Inhibitors: Emerging Priorities From Disproportionality Analysis of the FDA Adverse Event Reporting System. Target Oncol. 2019 Apr;14(2):205-221. doi: 10.1007/s11523-019-00632-w. [Article]
- FDA Approved Drug Products: Atezolizumab Intravenous Injection [Link]
- Roche News Release: Tecentriq as adjuvant treatment for NSCLC [Link]
- External Links
- KEGG Drug
- D10773
- PubChem Substance
- 347911207
- 1792776
- RxList
- RxList Drug Page
- Drugs.com
- Drugs.com Drug Page
- Wikipedia
- Atezolizumab
- FDA label
- Download (245 KB)
Clinical Trials
- Clinical Trials
Phase Status Purpose Conditions Count 4 Active Not Recruiting Treatment Malignancies 1 4 Active Not Recruiting Treatment Non-Small Cell Lung Carcinoma (NSCLC) 1 4 Not Yet Recruiting Treatment Hepatocellular Cancer (HCC) / Hepatocellular Carcinoma 1 4 Recruiting Diagnostic Malignant Lung Neoplasm 1 4 Recruiting Treatment Malignancies 1 3 Active Not Recruiting Treatment Abdominal wall neoplasm / Fallopian Tubes Cancer / Ovarian Cancer 1 3 Active Not Recruiting Treatment Breast Cancer 1 3 Active Not Recruiting Treatment Carcinoma of the Cervix, Stage IVB 1 3 Active Not Recruiting Treatment Castration Resistant Prostatic Neoplasms 1 3 Active Not Recruiting Treatment Hepatocellular Carcinoma 3
Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- Not Available
- Dosage Forms
Form Route Strength Injection, solution Intravenous 1200 mg/20mL Injection, solution Intravenous 840 mg/14mL Injection, solution, concentrate Intravenous Injection, solution, concentrate Intravenous 1200 mg Injection, solution, concentrate Intravenous 60 mg/1ml Injection, solution, concentrate Intravenous 840 mg Injection, solution, concentrate Intravenous; Parenteral 1200 MG Injection, solution, concentrate Intravenous; Parenteral 840 MG Solution Intravenous 1200 mg / 20 mL Solution Intravenous 840 mg / 14 mL Injection, solution, concentrate Solution Intravenous 1200 mg Solution Intravenous 840 mg/14ml - Prices
- Not Available
- Patents
- Not Available
Properties
- State
- Solid
- Experimental Properties
Property Value Source melting point (°C) 78 Ji-Hee, et al. Front Immunol, 7:394 (2016) boiling point (°C) Fab and Fc domains denaturates at 60 and 70 ºC respectively Arnoldus W. et al. (2000). Biophysical Journal. Vol 78. 394-404 water solubility 50mg/mL Human IgG purified. Product Information isoelectric point 6.6-7.2 Jin, et al. Electrophoresis. Sep;23(19):3385-91. (2002).
Targets
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- InhibitorAntibody
- General Function
- Not Available
- Specific Function
- Involved in the costimulatory signal, essential for T-cell proliferation and production of IL10 and IFNG, in an IL2-dependent and a PDCD1-independent manner. Interaction with PDCD1 inhibits T-cell ...
- Gene Name
- CD274
- Uniprot ID
- Q9NZQ7
- Uniprot Name
- Programmed cell death 1 ligand 1
- Molecular Weight
- 33275.095 Da
References
- Markham A: Atezolizumab: First Global Approval. Drugs. 2016 Aug;76(12):1227-32. doi: 10.1007/s40265-016-0618-8. [Article]
- Rosenberg JE, Hoffman-Censits J, Powles T, van der Heijden MS, Balar AV, Necchi A, Dawson N, O'Donnell PH, Balmanoukian A, Loriot Y, Srinivas S, Retz MM, Grivas P, Joseph RW, Galsky MD, Fleming MT, Petrylak DP, Perez-Gracia JL, Burris HA, Castellano D, Canil C, Bellmunt J, Bajorin D, Nickles D, Bourgon R, Frampton GM, Cui N, Mariathasan S, Abidoye O, Fine GD, Dreicer R: Atezolizumab in patients with locally advanced and metastatic urothelial carcinoma who have progressed following treatment with platinum-based chemotherapy: a single-arm, multicentre, phase 2 trial. Lancet. 2016 May 7;387(10031):1909-20. doi: 10.1016/S0140-6736(16)00561-4. Epub 2016 Mar 4. [Article]
- FDA Approved Drug Products: Atezolizumab Intravenous Injection [Link]
Drug created at May 19, 2016 15:42 / Updated at January 18, 2022 07:00