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.

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Associated Conditions

Contraindications & Blackbox Warnings

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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	inhibitor antibody	Humans
AProgrammed cell death protein 1	inhibitor	Humans

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 C_max was 0.27-0.35µg/mL/mg, and the C_min was 0.004-0.008µg/mL/mg.³

Volume of distribution

The volume of distribution of atezolizumab is 6.91L.^1,3

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

The half life of atezolizumab is 27 days.^1,3

Clearance

The clearance of atezolizumab is 0.200L/day.^1,3

Adverse Effects

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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 software
Abciximab	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.
Ambroxol	The risk or severity of methemoglobinemia can be increased when Atezolizumab is combined with Ambroxol.
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.

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Food Interactions

No interactions found.

Products

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Brand Name Prescription Products

Name	Dosage	Strength	Route	Labeller	Marketing Start	Marketing End
Tecentriq	Injection, solution, concentrate	1200 mg	Intravenous	Roche Registration Gmb H	2020-12-16	Not applicable
Tecentriq	Injection, solution	840 mg/14mL	Intravenous	Genentech, Inc.	2019-03-08	Not applicable
Tecentriq	Solution	840 mg / 14 mL	Intravenous	Hoffmann La Roche	2019-10-16	Not applicable
Tecentriq	Injection, solution	1200 mg/20mL	Intravenous	Genentech, Inc.	2016-05-18	Not applicable
Tecentriq	Injection, solution, concentrate	840 mg	Intravenous	Roche Registration Gmb H	2020-12-16	Not applicable
Tecentriq	Solution	1200 mg / 20 mL	Intravenous	Hoffmann La Roche	2017-05-02	Not applicable

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
RxNav: 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	Completed	Diagnostic	Lung Cancer	1
4	Completed	Treatment	Non-Small Cell Lung Carcinoma	1
4	Not Yet Recruiting	Treatment	Unresectable Hepatocellular Carcinoma (HCC)	1
4	Recruiting	Treatment	Cancer	1
4	Recruiting	Treatment	Hepatocellular Carcinoma / Liver Cancer	1
4	Recruiting	Treatment	Liver Cancer	1
3	Active Not Recruiting	Other	Invasive Breast Cancer	1
3	Active Not Recruiting	Treatment	Adenocarcinoma of Colon / DNA Repair-Deficiency Disorders / Lynch Syndrome / Stage III Colon Cancer AJCC v8	1
3	Active Not Recruiting	Treatment	Adenocarcinoma of Prostate / Metastatic Prostate Cancer	1
3	Active Not Recruiting	Treatment	Breast 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
Solution	Intravenous	840 mg/14ml
Solution	Intravenous	1200 mg

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

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Details1. Programmed cell death 1 ligand 1

Kind: Protein
Organism: Humans
Pharmacological action: Yes
Actions: Inhibitor
Antibody

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]

Details2. Programmed cell death protein 1

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

Atezolizumab

Identification

Pharmacology

Interactions

Products

Categories

Chemical Identifiers

References

Clinical Trials

Pharmacoeconomics

Properties

Targets

References

References