selpercatinib Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
tyrosine kinase inhibitors 5393 2152628-33-4

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • selpercatinib
  • retevmo
  • LOXO-292
  • LY3527723
Selpercatinib is a kinase inhibitor. Selpercatinib inhibited wild-type RET and multiple mutated RET isoforms as well as VEGFR1 and VEGFR3 with IC50 values ranging from 0.92 nM to 67.8 nM. In other enzyme assays, selpercatinib also inhibited FGFR 1, 2, and 3 at higher concentrations that were still clinically achievable. In cellular assays, selpercatinib inhibited RET at approximately 60-fold lower concentrations than FGFR1 and 2 and approximately 8-fold lower concentration than VEGFR3
  • Molecular weight: 525.61
  • Formula: C29H31N7O3
  • CLOGP: 2.82
  • LIPINSKI: 1
  • HAC: 10
  • HDO: 1
  • TPSA: 112.04
  • ALOGS: -4.25
  • ROTB: 8

  • Status: ONP

  • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

None

ADMET properties:

None

Approvals:

DateAgencyCompanyOrphan
Feb. 11, 2021 EMA Eli Lilly Nederland B.V.
May 8, 2020 FDA LOXO ONCOLOGY INC

FDA Adverse Event Reporting System (Female)

None

FDA Adverse Event Reporting System (Male)

None

Pharmacologic Action:

None

Drug Use (View source of the data)

DiseaseRelationSNOMED_IDDOID
Advanced RET fusion-positive non-small cell lung cancer indication 254637007 DOID:3908
Medullary thyroid carcinoma indication 255032005 DOID:3973
Metastasis from malignant tumor of thyroid indication 315007008
Advanced RET fusion-positive thyroid cancer indication 363478007 DOID:1781
Metastatic non-small cell lung cancer indication

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)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRouteExclusivity dateDescription
40MG RETEVMO LOXO ONCOLOGY INC N213246 May 8, 2020 RX CAPSULE ORAL May 8, 2025 NEW CHEMICAL ENTITY
80MG RETEVMO LOXO ONCOLOGY INC N213246 May 8, 2020 RX CAPSULE ORAL May 8, 2025 NEW CHEMICAL ENTITY
40MG RETEVMO LOXO ONCOLOGY INC N213246 May 8, 2020 RX CAPSULE ORAL May 8, 2027 ADULT AND PEDIATRIC PATIENTS 12 YEARS OF AGE AND OLDER WITH ADVANCED OR METASTATIC RET FUSION-POSITIVE THYROID CANCER WHO REQUIRE SYSTEMIC THERAPY AND WHO ARE RADIOACTIVE IODINE-REFRACTORY (IF RADIOACTIVE IODINE IS APPROPRIATE)
40MG RETEVMO LOXO ONCOLOGY INC N213246 May 8, 2020 RX CAPSULE ORAL May 8, 2027 INDICATED FOR THE TREATMENT OF ADULT AND PEDIATRIC PATIENTS 12 YEARS OF AGE AND OLDER WITH ADVANCED OR METASTATIC RET-MUTANT MEDULLARY THYROID CANCER (MTC) WHO REQUIRE SYSTEMIC THERAPY
40MG RETEVMO LOXO ONCOLOGY INC N213246 May 8, 2020 RX CAPSULE ORAL May 8, 2027 INDICATED FOR THE TREATMENT OF ADULT PATIENTS WITH METASTATIC RET FUSION-POSITIVE NON-SMALL CELL LUNG CANCER (NSCLC)
80MG RETEVMO LOXO ONCOLOGY INC N213246 May 8, 2020 RX CAPSULE ORAL May 8, 2027 ADULT AND PEDIATRIC PATIENTS 12 YEARS OF AGE AND OLDER WITH ADVANCED OR METASTATIC RET FUSION-POSITIVE THYROID CANCER WHO REQUIRE SYSTEMIC THERAPY AND WHO ARE RADIOACTIVE IODINE-REFRACTORY (IF RADIOACTIVE IODINE IS APPROPRIATE)
80MG RETEVMO LOXO ONCOLOGY INC N213246 May 8, 2020 RX CAPSULE ORAL May 8, 2027 INDICATED FOR THE TREATMENT OF ADULT AND PEDIATRIC PATIENTS 12 YEARS OF AGE AND OLDER WITH ADVANCED OR METASTATIC RET-MUTANT MEDULLARY THYROID CANCER (MTC) WHO REQUIRE SYSTEMIC THERAPY
80MG RETEVMO LOXO ONCOLOGY INC N213246 May 8, 2020 RX CAPSULE ORAL May 8, 2027 INDICATED FOR THE TREATMENT OF ADULT PATIENTS WITH METASTATIC RET FUSION-POSITIVE NON-SMALL CELL LUNG CANCER (NSCLC)

Bioactivity Summary:

None

External reference:

IDSource
D11713 KEGG_DRUG
4039392 VANDF
C4525531 UMLSCUI
Q6G PDB_CHEM_ID
CHEMBL4559134 ChEMBL_ID
C000656166 MESH_SUPPLEMENTAL_RECORD_UI
10318 IUPHAR_LIGAND_ID
10967 INN_ID
DB15685 DRUGBANK_ID
CEGM9YBNGD UNII
134436906 PUBCHEM_CID
2370147 RXNORM
334353 MMSL
38465 MMSL
d09562 MMSL
018362 NDDF
876841001 SNOMEDCT_US
876867006 SNOMEDCT_US

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
RETEVMO HUMAN PRESCRIPTION DRUG LABEL 1 0002-2980 CAPSULE 80 mg ORAL NDA 30 sections
RETEVMO HUMAN PRESCRIPTION DRUG LABEL 1 0002-3977 CAPSULE 40 mg ORAL NDA 30 sections