olaratumab 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
human origin 5183 1024603-93-7

Description:

MoleculeDescription

Synonyms:

  • olaratumab
  • lartruvo
  • IMC-3G3
  • IMC3G3
Olaratumab is a human IgG1 antibody that binds platelet-derived growth factor receptor alpha (PDGFR-alpha). PDGFR-alpha is a receptor tyrosine kinase expressed on cells of mesenchymal origin. Signaling through this receptor plays a role in cell growth, chemotaxis, and mesenchymal stem cell differentiation. The receptor has also been detected on some tumor and stromal cells, including sarcomas, where signaling can contribute to cancer cell proliferation, metastasis, and maintenance of the tumor microenvironment. The interaction between olaratumab and PDGFR-alpha prevents binding of the receptor by the PDGF-AA and -BB ligands as well as PDGF-AA, -BB, and -CC-induced receptor activation and downstream PDGFR-alpha pathway signaling. Olaratumab exhibits in vitro and in vivo anti-tumor activity against selected sarcoma cell lines and disrupted the PDGFR-alpha signaling pathway in in vivo tumor implant models.
  • Molecular weight:
  • Formula:
  • CLOGP:
  • LIPINSKI: None
  • HAC: None
  • HDO: None
  • TPSA:
  • ALOGS:
  • ROTB: None

Drug dosage:

None

ADMET properties:

None

Approvals:

DateAgencyCompanyOrphan
Nov. 9, 2016 EMA Eli Lilly Nederland B.V.
Oct. 19, 2016 FDA ELI LILLY AND CO

FDA Adverse Event Reporting System (Female)

None

FDA Adverse Event Reporting System (Male)

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
Neoplasm recurrence 66.74 52.18 12 258 2237 34954424

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
Febrile neutropenia 91.94 53.72 39 466 230960 79512923
Neoplasm recurrence 67.65 53.72 13 492 4201 79739682

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC L01FX10 ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS
ANTINEOPLASTIC AGENTS
MONOCLONAL ANTIBODIES AND ANTIBODY DRUG CONJUGATES
Other monoclonal antibodies and antibody drug conjugates
MeSH PA D000970 Antineoplastic Agents
FDA MoA N0000020028 Platelet-derived Growth Factor alpha Receptor Inhibitors
FDA EPC N0000193221 Platelet-derived Growth Factor Receptor alpha Antagonist

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

DiseaseRelationSNOMED_IDDOID
Sarcoma of soft tissue indication 424952003




🐶 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
Platelet-derived growth factor receptor alpha Kinase ANTIBODY BINDING Kd 10.40 IUPHAR DRUG LABEL

External reference:

IDSource
TT6HN20MVF UNII
4036148 VANDF
C2698152 UMLSCUI
CHEMBL1743049 ChEMBL_ID
D09939 KEGG_DRUG
DB06043 DRUGBANK_ID
9308 INN_ID
9172 IUPHAR_LIGAND_ID
1855735 RXNORM
244924 MMSL
32032 MMSL
d08482 MMSL
017019 NDDF
723523007 SNOMEDCT_US
763546008 SNOMEDCT_US
C000589393 MESH_SUPPLEMENTAL_RECORD_UI

Pharmaceutical products:

None