Atezolizumab
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 In November 2022, the manufacturer (Genentech) voluntarily withdrew the use of atezolizumab for the treatment of urothelial carcinoma, previously approved under the FDA's Accelerated Approval Program. The rest of atezolizumab indications remain unaffected.10
- 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 has approved indications for the following conditions:11
Non-Small Cell Lung Cancer (NSCLC)
- as adjuvant treatment following resection and platinum-based chemotherapy for adult patients with Stage II to IIIA NSCLC whose tumours have PD-L1 expression on ≥ 1% of tumour cells, as determined by an FDA-approved test.
- for the first-line treatment of adult patients with metastatic NSCLC whose tumours have high PD-L1 expression (PD-L1 stained ≥ 50% of tumour cells [TC ≥ 50%] or PD-L1 stained tumour-infiltrating immune cells [IC] covering ≥ 10% of the tumour area [IC ≥ 10%]), as determined by an FDAapproved test, with no EGFR or ALK genomic tumour aberrations.
- in combination with bevacizumab, paclitaxel, and carboplatin, for the first-line treatment of adult patients with metastatic non-squamous NSCLC with no EGFR or ALK genomic tumour aberrations.
- in combination with paclitaxel protein-bound and carboplatin for the firstline treatment of adult patients with metastatic non-squamous NSCLC with no EGFR or ALK genomic tumor aberrations.
- for the treatment of adult patients with metastatic NSCLC who have disease progression during or following platinum-containing chemotherapy. Patients with EGFR or ALK genomic tumour aberrations should have disease progression on FDA-approved therapy for NSCLC harbouring these aberrations prior to receiving atezolizumab.
Small Cell Lung Cancer (SCLC)
- in combination with carboplatin and etoposide, for the first-line treatment of adult patients with extensive-stage small cell lung cancer (ES-SCLC).
Hepatocellular Carcinoma (HCC)
- in combination with bevacizumab for the treatment of patients with unresectable or metastatic HCC who have not received prior systemic therapy.
Melanoma
- in combination with cobimetinib and vemurafenib for the treatment of patients with BRAF V600 mutation-positive unresectable or metastatic melanoma.
Alveolar Soft Part Sarcoma (ASPS)
- for the treatment of adult and pediatric patients 2 years of age and older with unresectable or metastatic ASPS.
Reduce drug development failure ratesBuild, train, & validate machine-learning modelswith evidence-based and structured datasets.Build, train, & validate predictive machine-learning models with structured datasets.- Associated Conditions
Indication Type Indication Combined Product Details Approval Level Age Group Patient Characteristics Dose Form Treatment of Metastatic alveolar soft part sarcoma •••••••••••• Used in combination to treat Metastatic hepatocellular carcinoma Regimen in combination with: Bevacizumab (DB00112) •••••••••••• ••••• ••••••••• ••••• Used in combination to treat Metastatic melanoma Regimen in combination with: Vemurafenib (DB08881), Cobimetinib (DB05239) •••••••••••• Treatment of Metastatic non-small cell lung cancer •••••••••••• ••••• ••••••••• ••••• ••••••••• Treatment of Metastatic non-squamous non small cell lung cancer •••••••••••• ••••• ••••••• ••••••••••• ••••• ••••••••••••••••••• •••••••••••• - Contraindications & Blackbox Warnings
- Prevent Adverse Drug Events TodayTap into our Clinical API for life-saving information on contraindications & blackbox warnings, population restrictions, harmful risks, & more.Avoid life-threatening adverse drug events with our Clinical API
- 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 AProgrammed cell death protein 1 inhibitorHumans - 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. View sample adverse effects data in our new Data Library!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 Browse all" title="About SNP Mediated Effects/ADRs" id="snp-actions-info" class="drug-info-popup" href="javascript:void(0);">
- Not Available
Interactions
- Drug Interactions Learn More" title="About Drug Interactions" id="structured-interactions-info" class="drug-info-popup" href="javascript:void(0);">
- 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. - Food Interactions
- 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 Injection, solution 840 mg/14mL Intravenous Genentech, Inc. 2019-03-08 Not applicable US Tecentriq Injection, solution, concentrate 1200 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 Tecentriq Solution 840 mg / 14 mL Intravenous Hoffmann La Roche 2019-10-16 Not applicable Canada Tecentriq Solution 1200 mg / 20 mL Intravenous Hoffmann La Roche 2017-05-02 Not applicable Canada
Categories
- ATC Codes
- L01FF05 — Atezolizumab
- Drug Categories
- Amino Acids, Peptides, and Proteins
- Antibodies
- Antibodies, Monoclonal
- Antibodies, Monoclonal, Humanized
- Antineoplastic Agents
- Antineoplastic Agents, Immunological
- Antineoplastic and Immunomodulating Agents
- Blood Proteins
- Cancer immunotherapy
- Globulins
- Immune Checkpoint Inhibitors
- Immunoglobulins
- Immunoproteins
- Immunotherapy
- MONOCLONAL ANTIBODIES AND ANTIBODY DRUG CONJUGATES
- Narrow Therapeutic Index Drugs
- PD-1/PDL-1 (Programmed cell death protein 1/death ligand 1) inhibitors
- 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]
- European Commission approves Roche’s Tecentriq as adjuvant treatment for a subset of people with early-stage non-small cell lung cancer [Link]
- BioSpace: Roche Withdraws Tecentriq for Bladder Cancer Indication [Link]
- FDA Approved Drug Products: TECENTRIQ (atezolizumab) injection, for intravenous use (December 2022_2) [Link]
- FDA Approved Drug Products: Tecentriq (atezolizumab) injection for intravenous use (May 2023) [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 Learn More" title="About Clinical Trials" id="clinical-trials-info" class="drug-info-popup" href="javascript:void(0);">
Phase Status Purpose Conditions Count 4 Completed Diagnostic Lung Cancer 1 4 Completed Treatment Non-Small Cell Lung Carcinoma 1 4 Not Yet Recruiting Treatment Infusion related reaction / Oncology 1 4 Not Yet Recruiting Treatment Unresectable Hepatocellular Carcinoma (HCC) 1 4 Recruiting Treatment Hepatocellular Carcinoma / Liver Cancer 1
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 1200.000 mg Solution Intravenous 840 mg / 14 mL Injection, solution, concentrate 1200 mg/20ml Injection, solution, concentrate 840 mg/14ml 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
![](https://go.drugbank.com/assets/locked/DrugTargets2-682eb846d210ae4bf33ca03febccfb57bb1c61318e699b729e5df4dfab2c5b67.png)
- 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]
- Kyriakidis I, Vasileiou E, Rossig C, Roilides E, Groll AH, Tragiannidis A: Invasive Fungal Diseases in Children with Hematological Malignancies Treated with Therapies That Target Cell Surface Antigens: Monoclonal Antibodies, Immune Checkpoint Inhibitors and CAR T-Cell Therapies. J Fungi (Basel). 2021 Mar 5;7(3). pii: jof7030186. doi: 10.3390/jof7030186. [Article]
- FDA Approved Drug Products: Atezolizumab Intravenous Injection [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Inhibitor
- General Function
- Signal transducer activity
- Specific Function
- Inhibitory cell surface receptor involved in the regulation of T-cell function during immunity and tolerance. Upon ligand binding, inhibits T-cell effector functions in an antigen-specific manner. ...
- Gene Name
- PDCD1
- Uniprot ID
- Q15116
- Uniprot Name
- Programmed cell death protein 1
- Molecular Weight
- 31646.635 Da
References
- Kyriakidis I, Vasileiou E, Rossig C, Roilides E, Groll AH, Tragiannidis A: Invasive Fungal Diseases in Children with Hematological Malignancies Treated with Therapies That Target Cell Surface Antigens: Monoclonal Antibodies, Immune Checkpoint Inhibitors and CAR T-Cell Therapies. J Fungi (Basel). 2021 Mar 5;7(3). pii: jof7030186. doi: 10.3390/jof7030186. [Article]
Drug created at May 19, 2016 15:42 / Updated at May 19, 2023 23:20