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

Stem definition	Drug id	CAS RN
tyrosine kinase inhibitors	5393	2152628-33-4

Description:

Molecule	Description
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: 3.21 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

Molecule

Description

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: 3.21
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:

Dose	Unit	Route
0.32	g	O

ADMET properties:

Property	Value	Reference
BDDCS (Biopharmaceutical Drug Disposition Classification System)	1	Bocci G, Oprea TI, Benet LZ

Approvals:

Date	Agency	Company
Feb. 11, 2021	EMA	Eli Lilly Nederland B.V.
May 8, 2020	FDA	LOXO ONCOLOGY INC
Sept. 27, 2021	PMDA	ELI LILLY JAPAN K.K.

FDA Adverse Event Reporting System (Female)

MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Tumour associated fever	69.53	62.56	9	267	333	63488413

FDA Adverse Event Reporting System (Male)

None

FDA Adverse Event Reporting System (Geriatric)

None

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

Source	Code	Description
ATC	L01EX22	ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS ANTINEOPLASTIC AGENTS PROTEIN KINASE INHIBITORS Other protein kinase inhibitors
FDA EPC	N0000175605	Kinase Inhibitor
FDA MoA	N0000185503	P-Glycoprotein Inhibitors
FDA MoA	N0000187062	Cytochrome P450 2C8 Inhibitors
FDA MoA	N0000190113	Breast Cancer Resistance Protein Inhibitors
FDA MoA	N0000190114	Cytochrome P450 3A Inhibitors
FDA MoA	N0000191423	Multidrug and Toxin Extrusion Transporter 1 Inhibitors
FDA MoA	N0000193947	Rearranged during Transfection (RET) Inhibitors

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

Disease	Relation	SNOMED_ID	DOID
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

🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

None

Orange Book patent data (new drug applications)

Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Patent number	Patent expiration date	Patent use
40MG	RETEVMO	LOXO ONCOL ELI LILLY	N213246	May 8, 2020	RX	CAPSULE	ORAL	10137124	Oct. 10, 2037	TREATMENT OF ADULT AND PEDIATRIC PATIENTS 12 YEARS OF AGE AND OLDER WITH ADVANCED OR METASTATIC MEDULLARY THYROID CANCER (MTC) WITH A RET MUTATION, AS DETECTED BY AN FDA-APPROVED TEST, WHO REQUIRE SYSTEMIC THERAPY
40MG	RETEVMO	LOXO ONCOL ELI LILLY	N213246	May 8, 2020	RX	CAPSULE	ORAL	10137124	Oct. 10, 2037	TREATMENT OF 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 ONCOL ELI LILLY	N213246	May 8, 2020	RX	CAPSULE	ORAL	10137124	Oct. 10, 2037	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 ONCOL ELI LILLY	N213246	May 8, 2020	RX	CAPSULE	ORAL	10137124	Oct. 10, 2037	TREATMENT OF ADULT AND PEDIATRIC PATIENTS 12 YEARS OF AGE AND OLDER WITH ADVANCED OR METASTATIC THYROID CANCER WITH A RET GENE FUSION, AS DETECTED BY AN FDA-APPROVED TEST, WHO REQUIRE SYSTEMIC THERAPY AND WHO ARE RADIOACTIVE IODINE-REFRACTORY
40MG	RETEVMO	LOXO ONCOL ELI LILLY	N213246	May 8, 2020	RX	CAPSULE	ORAL	10137124	Oct. 10, 2037	TREATMENT OF ADULT PATIENTS WITH LOCALLY ADVANCED OR METASTATIC NON-SMALL CELL LUNG CANCER (NSCLC) WITH A REARRANGED DURING TRANSFECTION (RET) GENE FUSION, AS DETECTED BY AN FDA-APPROVED TEST
40MG	RETEVMO	LOXO ONCOL ELI LILLY	N213246	May 8, 2020	RX	CAPSULE	ORAL	10137124	Oct. 10, 2037	TREATMENT OF ADULT PATIENTS WITH LOCALLY ADVANCED OR METASTATIC SOLID TUMORS WITH A RET GENE FUSION THAT HAVE PROGRESSED ON OR FOLLOWING PRIOR SYSTEMIC TREATMENT OR WHO HAVE NO SATISFACTORY ALTERNATIVE TREATMENT OPTIONS
40MG	RETEVMO	LOXO ONCOL ELI LILLY	N213246	May 8, 2020	RX	CAPSULE	ORAL	10137124	Oct. 10, 2037	TREATMENT OF ADULT PATIENTS WITH METASTATIC RET FUSION-POSITIVE NON-SMALL CELL LUNG CANCER
40MG	RETEVMO	LOXO ONCOL ELI LILLY	N213246	May 8, 2020	RX	CAPSULE	ORAL	10172851	Oct. 10, 2037	TREATMENT OF ADULT AND PEDIATRIC PATIENTS 12 YEARS OF AGE AND OLDER WITH ADVANCED OR METASTATIC MEDULLARY THYROID CANCER (MTC) WITH A RET MUTATION, AS DETECTED BY AN FDA-APPROVED TEST, WHO REQUIRE SYSTEMIC THERAPY
40MG	RETEVMO	LOXO ONCOL ELI LILLY	N213246	May 8, 2020	RX	CAPSULE	ORAL	10172851	Oct. 10, 2037	TREATMENT OF 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 ONCOL ELI LILLY	N213246	May 8, 2020	RX	CAPSULE	ORAL	10172851	Oct. 10, 2037	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 ONCOL ELI LILLY	N213246	May 8, 2020	RX	CAPSULE	ORAL	10172851	Oct. 10, 2037	TREATMENT OF ADULT AND PEDIATRIC PATIENTS 12 YEARS OF AGE AND OLDER WITH ADVANCED OR METASTATIC THYROID CANCER WITH A RET GENE FUSION, AS DETECTED BY AN FDA-APPROVED TEST, WHO REQUIRE SYSTEMIC THERAPY AND WHO ARE RADIOACTIVE IODINE-REFRACTORY
40MG	RETEVMO	LOXO ONCOL ELI LILLY	N213246	May 8, 2020	RX	CAPSULE	ORAL	10172851	Oct. 10, 2037	TREATMENT OF ADULT PATIENTS WITH LOCALLY ADVANCED OR METASTATIC NON-SMALL CELL LUNG CANCER (NSCLC) WITH A REARRANGED DURING TRANSFECTION (RET) GENE FUSION, AS DETECTED BY AN FDA-APPROVED TEST
40MG	RETEVMO	LOXO ONCOL ELI LILLY	N213246	May 8, 2020	RX	CAPSULE	ORAL	10172851	Oct. 10, 2037	TREATMENT OF ADULT PATIENTS WITH LOCALLY ADVANCED OR METASTATIC SOLID TUMORS WITH A RET GENE FUSION THAT HAVE PROGRESSED ON OR FOLLOWING PRIOR SYSTEMIC TREATMENT OR WHO HAVE NO SATISFACTORY ALTERNATIVE TREATMENT OPTIONS
40MG	RETEVMO	LOXO ONCOL ELI LILLY	N213246	May 8, 2020	RX	CAPSULE	ORAL	10172851	Oct. 10, 2037	TREATMENT OF ADULT PATIENTS WITH METASTATIC RET FUSION-POSITIVE NON-SMALL CELL LUNG CANCER
80MG	RETEVMO	LOXO ONCOL ELI LILLY	N213246	May 8, 2020	RX	CAPSULE	ORAL	10137124	Oct. 10, 2037	TREATMENT OF ADULT AND PEDIATRIC PATIENTS 12 YEARS OF AGE AND OLDER WITH ADVANCED OR METASTATIC MEDULLARY THYROID CANCER (MTC) WITH A RET MUTATION, AS DETECTED BY AN FDA-APPROVED TEST, WHO REQUIRE SYSTEMIC THERAPY
80MG	RETEVMO	LOXO ONCOL ELI LILLY	N213246	May 8, 2020	RX	CAPSULE	ORAL	10137124	Oct. 10, 2037	TREATMENT OF 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 ONCOL ELI LILLY	N213246	May 8, 2020	RX	CAPSULE	ORAL	10137124	Oct. 10, 2037	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 ONCOL ELI LILLY	N213246	May 8, 2020	RX	CAPSULE	ORAL	10137124	Oct. 10, 2037	TREATMENT OF ADULT AND PEDIATRIC PATIENTS 12 YEARS OF AGE AND OLDER WITH ADVANCED OR METASTATIC THYROID CANCER WITH A RET GENE FUSION, AS DETECTED BY AN FDA-APPROVED TEST, WHO REQUIRE SYSTEMIC THERAPY AND WHO ARE RADIOACTIVE IODINE-REFRACTORY
80MG	RETEVMO	LOXO ONCOL ELI LILLY	N213246	May 8, 2020	RX	CAPSULE	ORAL	10137124	Oct. 10, 2037	TREATMENT OF ADULT PATIENTS WITH LOCALLY ADVANCED OR METASTATIC NON-SMALL CELL LUNG CANCER (NSCLC) WITH A REARRANGED DURING TRANSFECTION (RET) GENE FUSION, AS DETECTED BY AN FDA-APPROVED TEST
80MG	RETEVMO	LOXO ONCOL ELI LILLY	N213246	May 8, 2020	RX	CAPSULE	ORAL	10137124	Oct. 10, 2037	TREATMENT OF ADULT PATIENTS WITH LOCALLY ADVANCED OR METASTATIC SOLID TUMORS WITH A RET GENE FUSION THAT HAVE PROGRESSED ON OR FOLLOWING PRIOR SYSTEMIC TREATMENT OR WHO HAVE NO SATISFACTORY ALTERNATIVE TREATMENT OPTIONS
80MG	RETEVMO	LOXO ONCOL ELI LILLY	N213246	May 8, 2020	RX	CAPSULE	ORAL	10137124	Oct. 10, 2037	TREATMENT OF ADULT PATIENTS WITH METASTATIC RET FUSION-POSITIVE NON-SMALL CELL LUNG CANCER
80MG	RETEVMO	LOXO ONCOL ELI LILLY	N213246	May 8, 2020	RX	CAPSULE	ORAL	10172851	Oct. 10, 2037	TREATMENT OF 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 ONCOL ELI LILLY	N213246	May 8, 2020	RX	CAPSULE	ORAL	10172851	Oct. 10, 2037	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 ONCOL ELI LILLY	N213246	May 8, 2020	RX	CAPSULE	ORAL	10172851	Oct. 10, 2037	TREATMENT OF ADULT PATIENTS WITH METASTATIC RET FUSION-POSITIVE NON-SMALL CELL LUNG CANCER
40MG	RETEVMO	LOXO ONCOL ELI LILLY	N213246	May 8, 2020	RX	CAPSULE	ORAL	10584124	Oct. 10, 2038	TREATMENT OF ADULT AND PEDIATRIC PATIENTS 12 YEARS OF AGE AND OLDER WITH ADVANCED OR METASTATIC MEDULLARY THYROID CANCER (MTC) WITH A RET MUTATION, AS DETECTED BY AN FDA-APPROVED TEST, WHO REQUIRE SYSTEMIC THERAPY
40MG	RETEVMO	LOXO ONCOL ELI LILLY	N213246	May 8, 2020	RX	CAPSULE	ORAL	10584124	Oct. 10, 2038	TREATMENT OF 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 ONCOL ELI LILLY	N213246	May 8, 2020	RX	CAPSULE	ORAL	10584124	Oct. 10, 2038	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 ONCOL ELI LILLY	N213246	May 8, 2020	RX	CAPSULE	ORAL	10584124	Oct. 10, 2038	TREATMENT OF ADULT AND PEDIATRIC PATIENTS 12 YEARS OF AGE AND OLDER WITH ADVANCED OR METASTATIC THYROID CANCER WITH A RET GENE FUSION, AS DETECTED BY AN FDA-APPROVED TEST, WHO REQUIRE SYSTEMIC THERAPY AND WHO ARE RADIOACTIVE IODINE-REFRACTORY
40MG	RETEVMO	LOXO ONCOL ELI LILLY	N213246	May 8, 2020	RX	CAPSULE	ORAL	10584124	Oct. 10, 2038	TREATMENT OF ADULT PATIENTS WITH LOCALLY ADVANCED OR METASTATIC NON-SMALL CELL LUNG CANCER (NSCLC) WITH A REARRANGED DURING TRANSFECTION (RET) GENE FUSION, AS DETECTED BY AN FDA-APPROVED TEST
40MG	RETEVMO	LOXO ONCOL ELI LILLY	N213246	May 8, 2020	RX	CAPSULE	ORAL	10584124	Oct. 10, 2038	TREATMENT OF ADULT PATIENTS WITH LOCALLY ADVANCED OR METASTATIC SOLID TUMORS WITH A RET GENE FUSION THAT HAVE PROGRESSED ON OR FOLLOWING PRIOR SYSTEMIC TREATMENT OR WHO HAVE NO SATISFACTORY ALTERNATIVE TREATMENT OPTIONS
40MG	RETEVMO	LOXO ONCOL ELI LILLY	N213246	May 8, 2020	RX	CAPSULE	ORAL	10584124	Oct. 10, 2038	TREATMENT OF ADULT PATIENTS WITH METASTATIC RET FUSION-POSITIVE NON-SMALL CELL LUNG CANCER
40MG	RETEVMO	LOXO ONCOL ELI LILLY	N213246	May 8, 2020	RX	CAPSULE	ORAL	10786489	Oct. 10, 2038	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 ONCOL ELI LILLY	N213246	May 8, 2020	RX	CAPSULE	ORAL	10786489	Oct. 10, 2038	THE TREATMENT OF ADULT PATIENTS WITH METASTATIC RET FUSION-POSITIVE NON-SMALL CELL LUNG CANCER (NSCLC)
40MG	RETEVMO	LOXO ONCOL ELI LILLY	N213246	May 8, 2020	RX	CAPSULE	ORAL	10786489	Oct. 10, 2038	TREATING ADULT AND PEDIATRIC PATIENTS 12 YEARS OF AGE AND OLDER WITH ADVANCED OR METASTATIC RET FUSION-POSITIVE REFRACTORY DIFFERENTIATED THYROID CANCER WHO REQUIRE SYSTEMIC THERAPY AND ARE RADIOACTIVE IODINE-REFRACTORY
40MG	RETEVMO	LOXO ONCOL ELI LILLY	N213246	May 8, 2020	RX	CAPSULE	ORAL	10786489	Oct. 10, 2038	TREATING 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, WHEREIN THE CANCER IS DIFFERENTIATED THYROID CANCER
40MG	RETEVMO	LOXO ONCOL ELI LILLY	N213246	May 8, 2020	RX	CAPSULE	ORAL	10786489	Oct. 10, 2038	TREATING 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, WHEREIN THE CANCER IS MEDULLARY THYROID CANCER
40MG	RETEVMO	LOXO ONCOL ELI LILLY	N213246	May 8, 2020	RX	CAPSULE	ORAL	10786489	Oct. 10, 2038	TREATING 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, WHEREIN THE CANCER IS PAPILLARY THYROID CANCER
40MG	RETEVMO	LOXO ONCOL ELI LILLY	N213246	May 8, 2020	RX	CAPSULE	ORAL	10786489	Oct. 10, 2038	TREATING 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, WHEREIN THE CANCER IS RECURRENT THYROID CANCER
40MG	RETEVMO	LOXO ONCOL ELI LILLY	N213246	May 8, 2020	RX	CAPSULE	ORAL	10786489	Oct. 10, 2038	TREATMENT OF ADULT AND PEDIATRIC PATIENTS 12 YEARS OF AGE AND OLDER WITH ADVANCED OR METASTATIC MEDULLARY THYROID CANCER (MTC) WITH A RET MUTATION, AS DETECTED BY AN FDA-APPROVED TEST, WHO REQUIRE SYSTEMIC THERAPY
40MG	RETEVMO	LOXO ONCOL ELI LILLY	N213246	May 8, 2020	RX	CAPSULE	ORAL	10786489	Oct. 10, 2038	TREATMENT OF ADULT AND PEDIATRIC PATIENTS 12 YEARS OF AGE AND OLDER WITH ADVANCED OR METASTATIC THYROID CANCER WITH A RET GENE FUSION, AS DETECTED BY AN FDA-APPROVED TEST, WHO REQUIRE SYSTEMIC THERAPY AND WHO ARE RADIOACTIVE IODINE-REFRACTORY
40MG	RETEVMO	LOXO ONCOL ELI LILLY	N213246	May 8, 2020	RX	CAPSULE	ORAL	10786489	Oct. 10, 2038	TREATMENT OF ADULT PATIENTS WITH LOCALLY ADVANCED OR METASTATIC NON-SMALL CELL LUNG CANCER (NSCLC) WITH A REARRANGED DURING TRANSFECTION (RET) GENE FUSION, AS DETECTED BY AN FDA-APPROVED TEST
40MG	RETEVMO	LOXO ONCOL ELI LILLY	N213246	May 8, 2020	RX	CAPSULE	ORAL	10786489	Oct. 10, 2038	TREATMENT OF ADULT PATIENTS WITH LOCALLY ADVANCED OR METASTATIC SOLID TUMORS WITH A RET GENE FUSION THAT HAVE PROGRESSED ON OR FOLLOWING PRIOR SYSTEMIC TREATMENT OR WHO HAVE NO SATISFACTORY ALTERNATIVE TREATMENT OPTIONS
80MG	RETEVMO	LOXO ONCOL ELI LILLY	N213246	May 8, 2020	RX	CAPSULE	ORAL	10584124	Oct. 10, 2038	TREATMENT OF ADULT AND PEDIATRIC PATIENTS 12 YEARS OF AGE AND OLDER WITH ADVANCED OR METASTATIC MEDULLARY THYROID CANCER (MTC) WITH A RET MUTATION, AS DETECTED BY AN FDA-APPROVED TEST, WHO REQUIRE SYSTEMIC THERAPY
80MG	RETEVMO	LOXO ONCOL ELI LILLY	N213246	May 8, 2020	RX	CAPSULE	ORAL	10584124	Oct. 10, 2038	TREATMENT OF 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 ONCOL ELI LILLY	N213246	May 8, 2020	RX	CAPSULE	ORAL	10584124	Oct. 10, 2038	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 ONCOL ELI LILLY	N213246	May 8, 2020	RX	CAPSULE	ORAL	10584124	Oct. 10, 2038	TREATMENT OF ADULT AND PEDIATRIC PATIENTS 12 YEARS OF AGE AND OLDER WITH ADVANCED OR METASTATIC THYROID CANCER WITH A RET GENE FUSION, AS DETECTED BY AN FDA-APPROVED TEST, WHO REQUIRE SYSTEMIC THERAPY AND WHO ARE RADIOACTIVE IODINE-REFRACTORY
80MG	RETEVMO	LOXO ONCOL ELI LILLY	N213246	May 8, 2020	RX	CAPSULE	ORAL	10584124	Oct. 10, 2038	TREATMENT OF ADULT PATIENTS WITH LOCALLY ADVANCED OR METASTATIC NON-SMALL CELL LUNG CANCER (NSCLC) WITH A REARRANGED DURING TRANSFECTION (RET) GENE FUSION, AS DETECTED BY AN FDA-APPROVED TEST
80MG	RETEVMO	LOXO ONCOL ELI LILLY	N213246	May 8, 2020	RX	CAPSULE	ORAL	10584124	Oct. 10, 2038	TREATMENT OF ADULT PATIENTS WITH LOCALLY ADVANCED OR METASTATIC SOLID TUMORS WITH A RET GENE FUSION THAT HAVE PROGRESSED ON OR FOLLOWING PRIOR SYSTEMIC TREATMENT OR WHO HAVE NO SATISFACTORY ALTERNATIVE TREATMENT OPTIONS
80MG	RETEVMO	LOXO ONCOL ELI LILLY	N213246	May 8, 2020	RX	CAPSULE	ORAL	10584124	Oct. 10, 2038	TREATMENT OF ADULT PATIENTS WITH METASTATIC RET FUSION-POSITIVE NON-SMALL CELL LUNG CANCER
80MG	RETEVMO	LOXO ONCOL ELI LILLY	N213246	May 8, 2020	RX	CAPSULE	ORAL	10786489	Oct. 10, 2038	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 ONCOL ELI LILLY	N213246	May 8, 2020	RX	CAPSULE	ORAL	10786489	Oct. 10, 2038	THE TREATMENT OF ADULT PATIENTS WITH METASTATIC RET FUSION-POSITIVE NON-SMALL CELL LUNG CANCER (NSCLC)
80MG	RETEVMO	LOXO ONCOL ELI LILLY	N213246	May 8, 2020	RX	CAPSULE	ORAL	10786489	Oct. 10, 2038	TREATING ADULT AND PEDIATRIC PATIENTS 12 YEARS OF AGE AND OLDER WITH ADVANCED OR METASTATIC RET FUSION-POSITIVE REFRACTORY DIFFERENTIATED THYROID CANCER WHO REQUIRE SYSTEMIC THERAPY AND ARE RADIOACTIVE IODINE-REFRACTORY
80MG	RETEVMO	LOXO ONCOL ELI LILLY	N213246	May 8, 2020	RX	CAPSULE	ORAL	10786489	Oct. 10, 2038	TREATING 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, WHEREIN THE CANCER IS DIFFERENTIATED THYROID CANCER
80MG	RETEVMO	LOXO ONCOL ELI LILLY	N213246	May 8, 2020	RX	CAPSULE	ORAL	10786489	Oct. 10, 2038	TREATING 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, WHEREIN THE CANCER IS MEDULLARY THYROID CANCER
80MG	RETEVMO	LOXO ONCOL ELI LILLY	N213246	May 8, 2020	RX	CAPSULE	ORAL	10786489	Oct. 10, 2038	TREATING 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, WHEREIN THE CANCER IS PAPILLARY THYROID CANCER
80MG	RETEVMO	LOXO ONCOL ELI LILLY	N213246	May 8, 2020	RX	CAPSULE	ORAL	10786489	Oct. 10, 2038	TREATING 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, WHEREIN THE CANCER IS RECURRENT THYROID CANCER
80MG	RETEVMO	LOXO ONCOL ELI LILLY	N213246	May 8, 2020	RX	CAPSULE	ORAL	10786489	Oct. 10, 2038	TREATMENT OF ADULT AND PEDIATRIC PATIENTS 12 YEARS OF AGE AND OLDER WITH ADVANCED OR METASTATIC MEDULLARY THYROID CANCER (MTC) WITH A RET MUTATION, AS DETECTED BY AN FDA-APPROVED TEST, WHO REQUIRE SYSTEMIC THERAPY
80MG	RETEVMO	LOXO ONCOL ELI LILLY	N213246	May 8, 2020	RX	CAPSULE	ORAL	10786489	Oct. 10, 2038	TREATMENT OF ADULT AND PEDIATRIC PATIENTS 12 YEARS OF AGE AND OLDER WITH ADVANCED OR METASTATIC THYROID CANCER WITH A RET GENE FUSION, AS DETECTED BY AN FDA-APPROVED TEST, WHO REQUIRE SYSTEMIC THERAPY AND WHO ARE RADIOACTIVE IODINE-REFRACTORY
80MG	RETEVMO	LOXO ONCOL ELI LILLY	N213246	May 8, 2020	RX	CAPSULE	ORAL	10786489	Oct. 10, 2038	TREATMENT OF ADULT PATIENTS WITH LOCALLY ADVANCED OR METASTATIC NON-SMALL CELL LUNG CANCER (NSCLC) WITH A REARRANGED DURING TRANSFECTION (RET) GENE FUSION, AS DETECTED BY AN FDA-APPROVED TEST
80MG	RETEVMO	LOXO ONCOL ELI LILLY	N213246	May 8, 2020	RX	CAPSULE	ORAL	10786489	Oct. 10, 2038	TREATMENT OF ADULT PATIENTS WITH LOCALLY ADVANCED OR METASTATIC SOLID TUMORS WITH A RET GENE FUSION THAT HAVE PROGRESSED ON OR FOLLOWING PRIOR SYSTEMIC TREATMENT OR WHO HAVE NO SATISFACTORY ALTERNATIVE TREATMENT OPTIONS

Orange Book exclusivity data (new drug applications)

Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Exclusivity date	Description
40MG	RETEVMO	LOXO ONCOL ELI LILLY	N213246	May 8, 2020	RX	CAPSULE	ORAL	May 8, 2025	NEW CHEMICAL ENTITY
80MG	RETEVMO	LOXO ONCOL ELI LILLY	N213246	May 8, 2020	RX	CAPSULE	ORAL	May 8, 2025	NEW CHEMICAL ENTITY
40MG	RETEVMO	LOXO ONCOL ELI LILLY	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 ONCOL ELI LILLY	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 ONCOL ELI LILLY	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 ONCOL ELI LILLY	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 ONCOL ELI LILLY	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 ONCOL ELI LILLY	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)
40MG	RETEVMO	LOXO ONCOL ELI LILLY	N213246	May 8, 2020	RX	CAPSULE	ORAL	Sept. 21, 2029	TREATMENT OF ADULT PATIENTS WITH LOCALLY ADVANCED NON-SMALL CELL LUNG CANCER (NSCLC) WITH A REARRANGED DURING TRANSFECTION (RET) GENE FUSION, AS DETECTED BY AN FDA-APPROVED TEST
40MG	RETEVMO	LOXO ONCOL ELI LILLY	N213246	May 8, 2020	RX	CAPSULE	ORAL	Sept. 21, 2029	TREATMENT OF ADULT PATIENTS WITH LOCALLY ADVANCED OR METASTATIC SOLID TUMORS WITH A RET GENE FUSION THAT HAVE PROGRESSED ON OR FOLLOWING PRIOR SYSTEMIC TREATMENT OR WHO HAVE NO SATISFACTORY ALTERNATIVE TREATMENT OPTIONS
80MG	RETEVMO	LOXO ONCOL ELI LILLY	N213246	May 8, 2020	RX	CAPSULE	ORAL	Sept. 21, 2029	TREATMENT OF ADULT PATIENTS WITH LOCALLY ADVANCED NON-SMALL CELL LUNG CANCER (NSCLC) WITH A REARRANGED DURING TRANSFECTION (RET) GENE FUSION, AS DETECTED BY AN FDA-APPROVED TEST
80MG	RETEVMO	LOXO ONCOL ELI LILLY	N213246	May 8, 2020	RX	CAPSULE	ORAL	Sept. 21, 2029	TREATMENT OF ADULT PATIENTS WITH LOCALLY ADVANCED OR METASTATIC SOLID TUMORS WITH A RET GENE FUSION THAT HAVE PROGRESSED ON OR FOLLOWING PRIOR SYSTEMIC TREATMENT OR WHO HAVE NO SATISFACTORY ALTERNATIVE TREATMENT OPTIONS

Bioactivity Summary:

Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Bioact source	MoA source
Proto-oncogene tyrosine-protein kinase receptor Ret	Kinase	P07949	RET_HUMAN	INHIBITOR	IC50	7.76	DRUG LABEL	DRUG LABEL
Vascular endothelial growth factor receptor 2	Kinase	P35968	VGFR2_HUMAN		IC50	7	CHEMBL
Aurora kinase B	Kinase	Q96GD4	AURKB_HUMAN	INHIBITOR	IC50	7.10	DRUG LABEL

External reference:

ID	Source
D11713	KEGG_DRUG
CEGM9YBNGD	UNII
C5235396	UMLSCUI
Q6G	PDB_CHEM_ID
CHEMBL4559134	ChEMBL_ID
134436906	PUBCHEM_CID
DB15685	DRUGBANK_ID
10318	IUPHAR_LIGAND_ID
018362	NDDF
876841001	SNOMEDCT_US
876867006	SNOMEDCT_US
4039392	VANDF
2370147	RXNORM
334353	MMSL
38465	MMSL
d09562	MMSL
C000656166	MESH_SUPPLEMENTAL_RECORD_UI
10967	INN_ID

Pharmaceutical products:

Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
RETEVMO	HUMAN PRESCRIPTION DRUG LABEL	1	0002-2980	CAPSULE	80 mg	ORAL	NDA	30 sections
RETEVMO	HUMAN PRESCRIPTION DRUG LABEL	1	0002-2980	CAPSULE	80 mg	ORAL	NDA	30 sections
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
RETEVMO	HUMAN PRESCRIPTION DRUG LABEL	1	0002-3977	CAPSULE	40 mg	ORAL	NDA	30 sections
RETEVMO	HUMAN PRESCRIPTION DRUG LABEL	1	0002-3977	CAPSULE	40 mg	ORAL	NDA	30 sections