dostarlimab 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |

Stem definitionDrug idCAS RN
primate origin 5451 2022215-59-2

Description:

MoleculeDescription

Molfile

Synonyms:

  • dostarlimab
  • dostarlimab-gxly
  • jemperli
  • TSR-042
  • WBP-285
Dostarlimab-gxly is a humanized monoclonal antibody of the IgG4 isotype that binds to the PD-1 receptor and blocks its interaction with PD-L1 and PD-L2, releasing PD-1 pathway-mediated inhibition of the immune response, including the anti-tumor immune response. In syngeneic mouse tumor models, blocking PD-1 activity resulted in decreased tumor growth. Binding of the PD-1 ligands, PD-L1 and PD-L2, to the PD-1 receptor found on T cells inhibits T-cell proliferation and cytokine production. Upregulation of PD-1 ligands occurs in some tumors, and signaling through this pathway can contribute to inhibition of active T-cell immune surveillance of tumors.
  • Molecular weight:
  • Formula:
  • CLOGP:
  • LIPINSKI: None
  • HAC: None
  • HDO: None
  • TPSA:
  • ALOGS:
  • ROTB: None

Drug dosage:

None

ADMET properties:

None

Predicted pharmacokinetic/toxicological properties (PK-AZ):

None

Approvals:

DateAgencyCompanyOrphan
April 21, 2021 EMA GlaxoSmithKline (Ireland) Limited
April 22, 2021 FDA GLAXOSMITHKLINE

FDA Adverse Event Reporting System (Female)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Malignant neoplasm progression 353.83 46.96 123 2145 106747 90519432
Rash maculo-papular 104.29 46.96 39 2229 40894 90585285
Hypothyroidism 101.26 46.96 41 2227 53086 90573093
Adrenal insufficiency 100.57 46.96 35 2233 29886 90596293
Toxic skin eruption 96.18 46.96 29 2239 15745 90610434
Thrombocytopenia 75.54 46.96 53 2215 208672 90417507
Acute polyneuropathy 71.41 46.96 12 2256 449 90625730
Anaemia 70.29 46.96 63 2205 352739 90273440
Immune-mediated lung disease 65.83 46.96 14 2254 1866 90624313
Hyperthyroidism 56.07 46.96 20 2248 18290 90607889
Neuropathy peripheral 54.70 46.96 37 2231 136933 90489246
Colitis 54.33 46.96 29 2239 69913 90556266
Myocarditis 49.64 46.96 17 2251 13789 90612390
Skin toxicity 48.00 46.96 14 2254 6765 90619414

FDA Adverse Event Reporting System (Male)

None

FDA Adverse Event Reporting System (Geriatric)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Malignant neoplasm progression 293.74 44.17 113 1955 174454 110412777
Hypothyroidism 86.81 44.17 37 2031 72862 110514369
Rash maculo-papular 86.17 44.17 37 2031 74185 110513046
Toxic skin eruption 80.61 44.17 27 2041 27488 110559743
Adrenal insufficiency 80.01 44.17 30 2038 42360 110544871
Acute polyneuropathy 68.79 44.17 12 2056 756 110586475
Immune-mediated lung disease 55.45 44.17 14 2054 5289 110581942
Neuropathy peripheral 53.07 44.17 36 2032 179241 110407990
Thrombocytopenia 52.73 44.17 47 2021 348838 110238393
Hyperthyroidism 49.03 44.17 19 2049 29242 110557989
Skin toxicity 48.58 44.17 15 2053 11768 110575463
Peritoneal neoplasm 48.56 44.17 7 2061 127 110587104
Anaemia 46.54 44.17 54 2014 547032 110040199
Colitis 46.53 44.17 27 2041 102296 110484935

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC L01FF07 ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS
ANTINEOPLASTIC AGENTS
MONOCLONAL ANTIBODIES AND ANTIBODY DRUG CONJUGATES
PD-1/PD-L1 (Programmed cell death protein 1/death ligand 1) inhibitors
MeSH PA D000970 Antineoplastic Agents
FDA MoA N0000191259 Programmed Death Receptor-1-directed Antibody Interactions
FDA EPC N0000191260 Programmed Death Receptor-1 Blocking Antibody
CHEBI has role CHEBI:35610 antineoplastic agent

Related Drugs by ATC class:

L01FF PD-1/PD-L1 (Programmed cell death protein 1/death ligand 1) inhibitors 11 drugs
atezolizumabavelumabcemiplimabdurvalumabnivolumabpembrolizumabretifanlimabserplulimabsugemalimabtislelizumabtoripalimab

Drug Use | Suggest Off label Use Form| |View source of the data|

DiseaseRelationSNOMED_IDDOID
Recurrent or advanced endometrial cancer indication 254878006 DOID:2871




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

None

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])		Mechanism
action		Bioact sourceMoA source
Programmed cell death protein 1 Membrane receptor ANTIBODY BINDING Kd 8.82 SCIENTIFIC LITERATURE DRUG LABEL

External reference:

IDSource
D11366 KEGG_DRUG
P0GVQ9A4S5 UNII
C5242455 UMLSCUI
CHEBI:757538 CHEBI
CHEMBL4298124 ChEMBL_ID
DB15627 DRUGBANK_ID
10787 INN_ID
C000719628 MESH_SUPPLEMENTAL_RECORD_UI
11518 IUPHAR_LIGAND_ID
1156877005 SNOMEDCT_US
1156880006 SNOMEDCT_US
4040426 VANDF
4040427 VANDF
345588 MMSL
39478 MMSL
d09732 MMSL
018705 NDDF
2539967 RXNORM

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Jemperli HUMAN PRESCRIPTION DRUG LABEL 1 0173-0898 INJECTION 50 mg INTRAVENOUS BLA 27 sections