Ipilimumab
Identification
- Name
- Ipilimumab
- Accession Number
- DB06186
- Description
Ipilimumab is a fully humanized IgG1 monoclonal antibody that blocks cytotoxic T lymphocyte antigen-4 (CTLA-4).5 Blocking CTLA-4 removes an inhibitory signal from reducing the activity of T lymphocytes.1,2,5 Ipilimumab was developed by Bristol-Myers Squibb and Medarex.5
Ipilimumab was granted FDA approval on 25 March 2011.5
- Type
- Biotech
- Groups
- Approved
- Biologic Classification
- Protein Based Therapies
Monoclonal antibody (mAb) - Protein Structure
- Protein Chemical Formula
- C6572H10126N1734O2080S40
- Protein Average Weight
- 148000.0 Da
- Sequences
>Ipilimumab heavy chain (patent appl. US20150283234) QVQLVESGGGVVQPGRSLRLSCAASGFTFSSYTMHWVRQAPGKGLEWVTFISYDGNNKYY ADSVKGRFTISRDNSKNTLYLQMNSLRAEDTAIYYCARTGWLGPFDYWGQGTLVTVSSAS TKGPSVFPLAPSSKSTSGGTAALGCLVKDYFPEPVTVSWNSGALTSGVHTFPAVLQSSGL YSLSSVVTVPSSSLGTQTYICNVNHKPSNTKVDKRVEPKSCDKTHTCPPCPAPELLGGPS VFLFPPKPKDTLMISRTPEVTCVVVDVSHEDPEVKFNWYVDGVEVHNAKTKPREEQYNST YRVVSVLTVLHQDWLNGKEYKCKVSNKALPAPIEKTISKAKGQPREPQVYTLPPSRDELT KNQVSLTCLVKGFYPSDIAVEWESNGQPENNYKTTPPVLDSDGSFFLYSKLTVDKSRWQQ GNVFSCSVMHEALHNHYTQKSLSLSPGK
>Ipilimumab light chain EIVLTQSPGTLSLSPGERATLSCRASQSVGSSYLAWYQQKPGQAPRLLIYGAFSRATGIP DRFSGSGSGTDFTLTISRLEPEDFAVYYCQQYGSSPWTFGQGTKVEIKRTVAAPSVFIFP PSDEQLKSGTASVVCLLNNFYPREAKVQWKVDNALQSGNSQESVTEQDSKDSTYSLSSTL TLSKADYEKHKVYACEVTHQGLSSPVTKSFNRGEC
Download FASTA Format- Synonyms
- Ipilimumab
- External IDs
- BMS-734016
- MDX-010
- MDX-101
- MDX-CTLA-4
- MOAB-CTLA-4
Pharmacology
- Indication
Ipilimumab is indicated to treat unresectable or metastatic melanoma, as an adjuvant in the treatment of cutaneous melanoma, to treat microsatellite-high or mismatch repair deficient metastatic colorectal cancer, or to treat hepatocellular carcinoma.5 Ipilimumab with nivolumab is indicated to treat advanced renal cell carcinoma.5
- Associated Conditions
- Contraindications & Blackbox Warnings
Learn about our commercial Contraindications & Blackbox Warnings data.
Learn More- Pharmacodynamics
Ipilimumab is a human IgG1 that binds CTLA-4, preventing 1 T-cell inhibition signal pathway.3 It has a long duration of action as it is given every 3 to 4 weeks.5 Patients should be counselled regarding the risk of immune-mediated adverse effects, infusion related reactions, and embryo-fetal toxicity.5
- Mechanism of action
Cytotoxic T-lymphocyte antigen-4 (CTLA-4) is an inhibitory molecule that competes with the stimulatory CD28 for binding to B7 on antigen presenting cells.3 CTLA-4 and CD28 are both presented on the surface of T-cells.3 Ipilimumab is a human IgG1 that binds CTLA-4, preventing the inhibition of T-cell mediated immune responses to tumors.3
Target Actions Organism ACytotoxic T-lymphocyte protein 4 inhibitorantibodyHumans - Absorption
Cmax was 65.8µg/mL for 2-6 year olds, 70.1µg/mL for 6-<12 year olds, and 73.3µg/mL in patients 12 years and older.5 Data regarding the AUC and Tmax of ipilumumab are not readily available.3,5
- Volume of distribution
The volume of distribution at steady-state of ipilimumab is 7.21L.3
- Protein binding
Data regarding the protein binding of ipilimumab is not readily available.5
- Metabolism
The metabolism of ipilimumab does not involve the cytochrome P450 enzyme system.5,6 Because ipilimumab is a protein, it is expected to be degraded into small peptides and amino acids by proteolytic enzymes.4
- Route of elimination
Data regarding the route of elimination of ipilimumab is not readily available.5
- Half-life
Ipilimumab has a half life of 14.7 days.3
- Clearance
Ipilimumab has a clearance of 15.3 mL/hr.3 Systemic clearance increases proportionally with body weight.6
- Adverse Effects
Learn about our commercial Adverse Effects data.
Learn More- Toxicity
Data regarding ipilumumab overdose is not readily available.5 However, the most common adverse reactions to ipilumumab are fatigue, diarrhea, pruritus, rash, and colitis.5
- Affected organisms
- Humans and other mammals
- 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 Unlock Additional DataAbacavir Abacavir may decrease the excretion rate of Ipilimumab which could result in a higher serum level. Abciximab The risk or severity of adverse effects can be increased when Abciximab is combined with Ipilimumab. Acarbose Acarbose may decrease the excretion rate of Ipilimumab which could result in a higher serum level. Aceclofenac Aceclofenac may decrease the excretion rate of Ipilimumab which could result in a higher serum level. Acemetacin Acemetacin may decrease the excretion rate of Ipilimumab which could result in a higher serum level. Acetaminophen Acetaminophen may decrease the excretion rate of Ipilimumab which could result in a higher serum level. Acetazolamide Acetazolamide may increase the excretion rate of Ipilimumab which could result in a lower serum level and potentially a reduction in efficacy. Acetylsalicylic acid Acetylsalicylic acid may decrease the excretion rate of Ipilimumab which could result in a higher serum level. Aclidinium Ipilimumab may decrease the excretion rate of Aclidinium which could result in a higher serum level. Acrivastine Ipilimumab may decrease the excretion rate of Acrivastine which could result in a higher serum level. Additional Data Available- Extended DescriptionExtended DescriptionAvailable for Purchase
Extended description of the mechanism of action and particular properties of each drug interaction.
Learn more - SeveritySeverityAvailable for Purchase
A severity rating for each drug interaction, from minor to major.
Learn more - Evidence LevelEvidence LevelAvailable for Purchase
A rating for the strength of the evidence supporting each drug interaction.
Learn more - ActionActionAvailable for Purchase
An effect category for each drug interaction. Know how this interaction affects the subject drug.
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- Food Interactions
- No interactions found.
Products
Purchasing individual compounds or compound libraries for your research?
Learn More- International/Other Brands
- Yervoy
- Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Unlock Additional DataYervoy Injection 5 mg/1mL Intravenous E.R. Squibb & Sons, L.L.C. 2011-03-25 Not applicable US 
Yervoy Injection 5 mg/1mL Intravenous Baxter Pharmaceutical Solutions, LLC 2011-03-25 2016-04-11 US Yervoy Injection 5 mg/1mL Intravenous E.R. Squibb & Sons, L.L.C. 2011-03-25 Not applicable US Yervoy Liquid Intravenous Bristol Myers Squibb 2012-03-08 Not applicable Canada 
Yervoy Injection 5 mg/1mL Intravenous Baxter Pharmaceutical Solutions, LLC 2011-03-25 2016-04-11 US Additional Data Available- Application NumberApplication NumberAvailable for Purchase
A unique ID assigned by the FDA when a product is submitted for approval by the labeller.
Learn more - Product CodeProduct CodeAvailable for Purchase
A governmentally-recognized ID which uniquely identifies the product within its regulatory market.
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Categories
- ATC Codes
- L01XC11 — Ipilimumab
- Drug Categories
- Adjuvants, Immunologic
- Amino Acids, Peptides, and Proteins
- Antibodies
- Antibodies, Monoclonal
- Antibodies, Monoclonal, Humanized
- Antineoplastic Agents
- Antineoplastic Agents, Immunological
- Antineoplastic and Immunomodulating Agents
- Blood Proteins
- CTLA-4-directed Antibody Interactions
- CTLA-4-directed Blocking Antibody
- Drugs that are Mainly Renally Excreted
- Globulins
- Immune Checkpoint Inhibitors
- Immunoglobulin G
- Immunoglobulins
- Immunoproteins
- Increased T Lymphocyte Activation
- Narrow Therapeutic Index Drugs
- 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
Chemical Identifiers
- UNII
- 6T8C155666
- CAS number
- 477202-00-9
References
- General References
- Johnson DB, Peng C, Abramson RG, Ye F, Zhao S, Wolchok JD, Sosman JA, Carvajal RD, Ariyan CE: Clinical Activity of Ipilimumab in Acral Melanoma: A Retrospective Review. Oncologist. 2015 Jun;20(6):648-52. doi: 10.1634/theoncologist.2014-0468. Epub 2015 May 11. [PubMed:25964307]
- Thumar JR, Kluger HM: Ipilimumab: a promising immunotherapy for melanoma. Oncology (Williston Park). 2010 Dec;24(14):1280-8. [PubMed:21294471]
- Trinh VA, Hagen B: Ipilimumab for advanced melanoma: a pharmacologic perspective. J Oncol Pharm Pract. 2013 Sep;19(3):195-201. doi: 10.1177/1078155212459100. Epub 2012 Oct 9. [PubMed:23047236]
- Fellner C: Ipilimumab (yervoy) prolongs survival in advanced melanoma: serious side effects and a hefty price tag may limit its use. P T. 2012 Sep;37(9):503-30. [PubMed:23066344]
- FDA Approved Drug Products: Yervoy Ipilimumab Intravenous Injection [Link]
- BC Cancer Agency: Yervoy Monograph [Link]
- External Links
- KEGG Drug
- D04603
- PubChem Substance
- 347910341
- 1094833
- ChEMBL
- CHEMBL1789844
- RxList
- RxList Drug Page
- Drugs.com
- Drugs.com Drug Page
- Wikipedia
- Ipilimumab
- AHFS Codes
- 10:00.00 — Antineoplastic Agents
- FDA label
- Download (1.13 MB)
- MSDS
- Download (479 KB)
Clinical Trials
- Clinical Trials
Phase Status Purpose Conditions Count 4 Active Not Recruiting Treatment Lung Cancers 1 4 Active Not Recruiting Treatment Melanoma, Malignant 1 4 Active Not Recruiting Treatment Renal Cell Adenocarcinoma 1 4 Not Yet Recruiting Treatment Renal Cancers 1 4 Terminated Treatment Metastatic Melanoma 1 3 Active Not Recruiting Treatment Advanced Non Small Cell Lung Cancer 1 3 Active Not Recruiting Treatment Advanced Renal Cell Carcinoma / Metastatic Renal Cell Carcinoma 1 3 Active Not Recruiting Treatment Gastroesophageal Junction Cancer / Malignant Neoplasm of Stomach 1 3 Active Not Recruiting Treatment Head and Neck Carcinoma 1 3 Active Not Recruiting Treatment Lung Cancers 1
Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- Not Available
- Dosage Forms
Form Route Strength Injection Intravenous 5 mg/1mL Injection, solution, concentrate Intravenous; Parenteral 5 MG/ML Liquid Intravenous Injection, solution, concentrate Intravenous 200 mg/40mL Injection, solution, concentrate Intravenous 50 mg/10mL Solution Intravenous 50 mg - Prices
- Not Available
- Patents
Patent Number Pediatric Extension Approved Expires (estimated) Region Unlock Additional DataCA2381770 No 2007-08-07 2020-08-08 Canada Additional Data Available- Filed OnFiled OnAvailable for Purchase
The date on which a patent was filed with the relevant government.
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Properties
- State
- Liquid
- Experimental Properties
Property Value Source melting point (°C) 80-90 ºC (based on IgG properties) McConnell A., et al. (2014). MAbs. Sep-Oct; 6 (5); 1274-1282 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 50 mg/ml Human IgG purified. Product Information isoelectric point 6.1-8.5 Agrisera Information about IgG antibodies.
Targets
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- InhibitorAntibody
- General Function
- Not Available
- Specific Function
- Inhibitory receptor acting as a major negative regulator of T-cell responses. The affinity of CTLA4 for its natural B7 family ligands, CD80 and CD86, is considerably stronger than the affinity of t...
- Gene Name
- CTLA4
- Uniprot ID
- P16410
- Uniprot Name
- Cytotoxic T-lymphocyte protein 4
- Molecular Weight
- 24655.63 Da
References
- Yang JC, Hughes M, Kammula U, Royal R, Sherry RM, Topalian SL, Suri KB, Levy C, Allen T, Mavroukakis S, Lowy I, White DE, Rosenberg SA: Ipilimumab (anti-CTLA4 antibody) causes regression of metastatic renal cell cancer associated with enteritis and hypophysitis. J Immunother. 2007 Nov-Dec;30(8):825-30. [PubMed:18049334]
Drug created on March 19, 2008 10:16 / Updated on November 27, 2020 08:19
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