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
References:
  1. NIH Inxight Drugs: Toripalimab [Link]
Download FASTA Format
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

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Associated Conditions
Indication TypeIndicationCombined Product DetailsApproval LevelAge GroupPatient CharacteristicsDose Form
Treatment ofMetastatic nasopharyngeal carcinoma (npc)•••••••••••••••••••••••• ••••••••••• •• •• ••••• •••••••••••••• •••••••••••••••••••••
Used in combination to treatMetastatic nasopharyngeal carcinoma (npc)Regimen in combination with: Cisplatin (DB00515), Gemcitabine (DB00441)••••••••••••••••••••••••••
Used in combination to treatRecurrent, locally advanced nasopharyngeal carcinoma (npc)Regimen in combination with: Cisplatin (DB00515), Gemcitabine (DB00441)••••••••••••••••••••••••••
Treatment ofRecurrent, unresectable nasopharyngeal carcinoma (npc)•••••••••••••••••••••••• ••••••••••• •• •• ••••• •••••••••••••• •••••••••••••••••••••
Contraindications & Blackbox Warnings
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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

TargetActionsOrganism
UProgrammed cell death protein 1
inhibitor
antibody
Humans
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
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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.
DrugInteraction
AbciximabThe risk or severity of adverse effects can be increased when Abciximab is combined with Toripalimab.
AdalimumabThe risk or severity of adverse effects can be increased when Adalimumab is combined with Toripalimab.
AducanumabThe risk or severity of adverse effects can be increased when Aducanumab is combined with Toripalimab.
AlemtuzumabThe risk or severity of adverse effects can be increased when Alemtuzumab is combined with Toripalimab.
AlirocumabThe risk or severity of adverse effects can be increased when Alirocumab is combined with Toripalimab.
Food Interactions
Not Available

Products

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Brand Name Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
LoqtorziInjection240 mg/6mLIntravenousSuzhou Union Biopharm Co., Ltd.2023-10-27Not applicableUS flag
LoqtorziInjection240 mg/6mLIntravenousCoherus Biosciences, Inc.2023-10-27Not applicableUS flag

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
  1. 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]
  2. 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]
  3. Keam SJ: Toripalimab: First Global Approval. Drugs. 2019 Apr;79(5):573-578. doi: 10.1007/s40265-019-01076-2. [Article]
  4. FDA Approved Drug Products: Loqtorzi (toripalimab-tpzi) for intravenous injection [Link]
  5. US Food & Drug Administration: FDA approves toripalimab-tpzi for nasopharyngeal carcinoma [Link]
RxNav
2669406
Wikipedia
Toripalimab

Clinical Trials

Clinical Trials

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage Forms
FormRouteStrength
InjectionIntravenous240 mg/6mL
Prices
Not Available
Patents
Not Available

Properties

State
Liquid
Experimental Properties
Not Available

Targets

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Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Inhibitor
Antibody
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
  1. 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