Toripalimab
Identification
- Summary
Toripalimab is a PD-1 blocking monoclonal antibody used for the treatment of metastatic and recurrent nasopharyngeal carcinomas.
- Brand Names
- Loqtorzi
- Generic Name
- Toripalimab
- DrugBank Accession Number
- DB15043
- Background
The proliferation of some cancers can be attributed, at least in part, to the suppression of host tumor surveillance. One mechanism by which this occurs is through the overexpression of programmed cell death ligand (PD-L1)2 - the binding of PD-L1 (and PD-L2) to its target receptor (PD-1) results in the inhibition of T-cell proliferation and cytokine production, and thus its overexpression can inhibit T-cell-mediated immune surveillance of tumors.4
Toripalimab is a selective, recombinant, humanized IgG4 monoclonal antibody targeted against the PD-1 receptor. It was first approved in China in December 2018 for the treatment of unresectable or metastatic melanoma in previously treated patients.1,3 Toripalimab was granted FDA approval in October 2023 for the treatment of select patients with nasopharyngeal carcinomas.5
- Type
- Biotech
- Groups
- Approved, Investigational
- Biologic Classification
- Protein Based Therapies
Monoclonal antibody (mAb) - Protein Chemical Formula
- Not Available
- Protein Average Weight
- 150000.0 Da
- Sequences
>heavy_chain QGQLVQSGAEVKKPGASVKVSCKASGYTFTDYEMHWVRQAPIHGLEWIGVIESETGGTAY NQKFKGRVTITADKSTSTAYMELSSLRSEDTAVYYCAREGITTVATTYYWYFDVWGQGTT VTVSSASTKGPSVFPLAPCSRSTSESTAALGCLVKDYFPEPVTVSWNSGALTSGVHTFPA VLQSSGLYSLSSVVTVPSSSLGTKTYTCNVDHKPSNTKVDKRVESKYGPPCPPCPAPEFL GGPSVFLFPPKPKDTLMISRTPEVTCVVVDVSQEDPEVQFNWYVDGVEVHNAKTKPREEQ FNSTYRVVSVLTVLHQDWLNGKEYKCKVSNKGLPSSIEKTISKAKGQPREPQVYTLPPSQ EEMTKNQVSLTCLVKGFYPSDIAVEWESNGQPENNYKTTPPVLDSDGSFFLYSRLTVDKS RWQEGNVFSCSVMHEALHNHYTQKSLSLSLGK
>light_chain DVVMTQSPLSLPVTLGQPASISCRSSQSIVHSNGNTYLEWYLQKPGQSPQLLIYKVSNRF SGVPDRFSGSGSGTDFTLKISRVEAEDVGVYYCFQGSHVPLTFGQGTKLEIKRTVAAPSV FIFPPSDEQLKSGTASVVCLLNNFYPREAKVQWKVDNALQSGNSQESVTEQDSKDSTYSL SSTLTLSKADYEKHKVYACEVTHQGLSSPVTKSFNRGEC
Download FASTA FormatReferences:
- NIH Inxight Drugs: Toripalimab [Link]
- Synonyms
- Toripalimab
- External IDs
- JS 001
- JS-001
- JS001
Pharmacology
- Indication
Toripalimab is indicated in combination with cisplatin and gemcitabine for the first-line treatment of adult patients with metastatic or recurrent locally advanced nasopharyngeal carcinoma (NPC).4 It is also indicated as a second-line monotherapy for the treatment of adults with recurrent unresectable or metastatic NPC with disease progression on or after platinum-containing chemotherapy.4
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 nasopharyngeal carcinoma (npc) •••••••••••• ••••• ••••••• ••••••••••• •• •• ••••• •••••••••••••• •••••••••••• ••••••••• Used in combination to treat Metastatic nasopharyngeal carcinoma (npc) Regimen in combination with: Cisplatin (DB00515), Gemcitabine (DB00441) •••••••••••• ••••• ••••••••• Used in combination to treat Recurrent, locally advanced nasopharyngeal carcinoma (npc) Regimen in combination with: Cisplatin (DB00515), Gemcitabine (DB00441) •••••••••••• ••••• ••••••••• Treatment of Recurrent, unresectable nasopharyngeal carcinoma (npc) •••••••••••• ••••• ••••••• ••••••••••• •• •• ••••• •••••••••••••• •••••••••••• ••••••••• - 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
The exposure-response relationships and time course of pharmacodynamic response for toripalimab have not been fully characterized.4 In syngeneic mouse tumor models, blocking PD-1 activity resulted in decreased tumor growth.4
- Mechanism of action
The binding of programmed death ligands 1 and 2 (PD-L1 and PD-L2) to the PD-1 receptor on T-cells results in the inhibition of T-cell proliferation and cytokine production4 - this pathway therefore plays a vital role in immune inhibition and self-tolerance.2 In some cancers, PD-1 ligands may be overexpressed and result in the inhibition of tumor surveillance.4,2
Toripalimab is a monoclonal antibody directed against the PD-1 receptor. It blocks the PD-L1/PD-1 pathway, releasing PD-1 pathway-mediated inhibition of the immune response, including the anti-tumor immune response.4
Target Actions Organism UProgrammed cell death protein 1 inhibitorantibodyHumans - Absorption
Steady-state concentrations of toripalimab were reached by week 7 when administered every two weeks.4
- Volume of distribution
At steady-state, the mean volume of distribution was 3.7 L.4
- Protein binding
Not Available
- Metabolism
As with other therapeutic proteins, toripalimab is likely degraded via catabolic processes into smaller peptides and amino acids.4
- Route of elimination
Not Available
- Half-life
The mean terminal elimination half-life after one dose of toripalimab was 10 ± 1.5 days.4 The mean terminal elimination half-life of toripalimab at steady-state was 18 ± 9.4 days.4
- Clearance
The mean clearance after one dose of toripalimab was 14.9 mL/h.4 The mean clearance of toripalimab at steady-state was 9.5 mL/h.4
- 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
Not Available
- 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 Toripalimab. Adalimumab The risk or severity of adverse effects can be increased when Adalimumab is combined with Toripalimab. Aducanumab The risk or severity of adverse effects can be increased when Aducanumab is combined with Toripalimab. Alemtuzumab The risk or severity of adverse effects can be increased when Alemtuzumab is combined with Toripalimab. Alirocumab The risk or severity of adverse effects can be increased when Alirocumab is combined with Toripalimab. - Food Interactions
- Not Available
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 Loqtorzi Injection 240 mg/6mL Intravenous Suzhou Union Biopharm Co., Ltd. 2023-10-27 Not applicable US Loqtorzi Injection 240 mg/6mL Intravenous Coherus Biosciences, Inc. 2023-10-27 Not applicable US
Categories
- Drug Categories
- 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
- Humans
Chemical Identifiers
- UNII
- 8JXN261VVA
- CAS number
- 1924598-82-2
References
- General References
- Zhang L, Hao B, Geng Z, Geng Q: Toripalimab: the First Domestic Anti-Tumor PD-1 Antibody in China. Front Immunol. 2022 Jan 12;12:730666. doi: 10.3389/fimmu.2021.730666. eCollection 2021. [Article]
- Han Y, Liu D, Li L: PD-1/PD-L1 pathway: current researches in cancer. Am J Cancer Res. 2020 Mar 1;10(3):727-742. eCollection 2020. [Article]
- Keam SJ: Toripalimab: First Global Approval. Drugs. 2019 Apr;79(5):573-578. doi: 10.1007/s40265-019-01076-2. [Article]
- FDA Approved Drug Products: Loqtorzi (toripalimab-tpzi) for intravenous injection [Link]
- US Food & Drug Administration: FDA approves toripalimab-tpzi for nasopharyngeal carcinoma [Link]
- External Links
- 2669406
- Wikipedia
- Toripalimab
Clinical Trials
- Clinical Trials
Phase Status Purpose Conditions Count 4 Not Yet Recruiting Treatment Breast Cancer 1 3 Active Not Recruiting Treatment Advanced Hepatocellular Carcinoma (HCC) 2 3 Active Not Recruiting Treatment Advanced or Metastatic Esophageal Squamous Cell Cancer Without Previous Systemic Chemotherapy 1 3 Active Not Recruiting Treatment Metastatic Melanoma / Unresectable Melanoma 1 3 Active Not Recruiting Treatment Primary Disease: Unresectable or Metastatic Renal Cell Carcinoma Focus of the Study:PFS Assessed by IRC Per RECIST 1.1 1
Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- Not Available
- Dosage Forms
Form Route Strength Injection Intravenous 240 mg/6mL - Prices
- Not Available
- Patents
- Not Available
Properties
- State
- Liquid
- Experimental Properties
- Not Available
Targets
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- InhibitorAntibody
- 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
- FDA Approved Drug Products: Loqtorzi (toripalimab-tpzi) for intravenous injection [Link]
Drug created at May 20, 2019 14:44 / Updated at December 09, 2023 17:37