Selpercatinib
Highest phase reached
Approved
Drug type
Small molecule
First approval year
2020
- First approval year
- 2020
- Listing at source
- Listed
- Highest phase reached
- Approved
- Drug type
- Small molecule
- Drug name
- Selpercatinib
- Molecular weight
- 525.61
- Structure (SMILES)
- COc1ccc(CN2C3CC2CN(c2ccc(-c4cc(OCC(C)(C)O)cn5ncc(C#N)c45)cn2)C3)cn1
- retevmo
- Retevmo
- retsevmo
- Retsevmo
- loxo 292
- Loxo-292
- LOXO-292
- ly 3527723
- LY-3527723
- ly3527723
- LY3527723
- ret inhibitor loxo 292
- Ret inhibitor loxo-292
- selpercatinib
- Selpercatinib
- selpercatinib [INN]
- SELPERCATINIB [JAN]
- SELPERCATINIB [MI]
- SELPERCATINIB [ORANGE BOOK]
- SELPERCATINIB [USAN]
- Selpercatinib [WHO-DD]
- selpercatinib inn
- selpercatinib jan
- selpercatinib mi
- selpercatinib orange book
- selpercatinib usan
- selpercatinib who dd
- ATC classification codes
- L01EX22
Sources for recorded values
- CAS registry numbers
- 2152628-33-4
- ChEMBL ID
- CHEMBL4559134
- InChIKey
- XIIOFHFUYBLOLW-UHFFFAOYSA-N
- RxNorm IDs (RxCUI)
- 2370147
- FDA ingredient codes (UNII)
- CEGM9YBNGD
- 134436906
- 155804485
- Applicant
- ELI LILLY AND CO
- Approval date
- 8 May 2020
- Application number
- NDA213246
- Status
- Authorised
- Status date
- 11 Feb 2021
- Authorisation date
- 11 Feb 2021
- Approved indications
- Retsevmo as monotherapy is indicated for the treatment of adults with: advanced RET fusion positive non small cell lung cancer (NSCLC) not previously treated with a RET inhibitor. For biomarker-based patient selection, see section 4.2. Retsevmo as monotherapy is indicated for the treatment of adults and paediatric patients 2 years of age and older with: advanced RET fusion positive thyroid cancer who are radioactive iodine-refractory (if radioactive iodine is appropriate) . For biomarker-based patient selection, see section 4.2. advanced RET mutant medullary thyroid cancer (MTC) . For biomarker-based patient selection, see section 4.2. advanced RET fusion positive solid tumours, when treatment options not targeting RET provide limited clinical benefit, or have been exhausted (see sections 4.4 and 5.1). For biomarker-based patient selection, see section 4.2.
- Product number
- EMEA/H/C/005375
- Authorisation holder
- Eli Lilly Nederland B.V.
- Priority medicines scheme
- No
- Generic
- No
- Biosimilar
- No
- Generic medicines
- 0
- Biosimilar medicines
- 0
- Advanced therapy
- No
- Conditional approval
- No
- Additional monitoring
- No
- Accelerated assessment
- No
- Exceptional circumstances
- No
Therapeutic areas
- Cancer
- Carcinoma, Non-Small-Cell Lung
- Thyroid Neoplasms
European medicines record
- Patents
- 20
- Designations
- 7
- Earliest recorded loss of exclusivity
- 10 Apr 2039
- First in class
- No
- Fast track
- No
- Breakthrough designation
- Yes
- Orphan designation
- No
- Priority review
- Yes
- Orphan exclusivity
- No
- Accelerated approval
- Yes
- Availability
- Prescription only
- Pharmacology name
- selpercatinib
- Type
- Synthetic organic
- Drug name stem
- -tinib
- Approval recorded by Guide to Pharmacology
- Yes
Administration routes
- Oral
- Action
- Inhibition
- Action type
- Inhibitor
- Target
- ret proto-oncogene
- Gene symbol
- RET
- Protein identifier
- P07949
- Median affinity
- 7.85
- Affinity units
- pIC50
- Mechanism
- Coiled-coil domain-containing protein 6/Tyrosine-protein kinase receptor RET inhibitor
- Action type
- Inhibitor
- Target
- Coiled-coil domain-containing protein 6/Tyrosine-protein kinase receptor RET
- Protein identifier
- P07949
- Mechanism
- Coiled-coil domain-containing protein 6/Tyrosine-protein kinase receptor RET inhibitor
- Action type
- Inhibitor
- Target
- Coiled-coil domain-containing protein 6/Tyrosine-protein kinase receptor RET
- Protein identifier
- Q16204
- Mechanism
- Kinesin-1 heavy chain/ Tyrosine-protein kinase receptor RET inhibitor
- Action type
- Inhibitor
- Target
- Kinesin-1 heavy chain/ Tyrosine-protein kinase receptor RET
- Protein identifier
- P07949
- Mechanism
- Kinesin-1 heavy chain/ Tyrosine-protein kinase receptor RET inhibitor
- Action type
- Inhibitor
- Target
- Kinesin-1 heavy chain/ Tyrosine-protein kinase receptor RET
- Protein identifier
- P33176
- Mechanism
- Tyrosine-protein kinase receptor RET inhibitor
- Action type
- Inhibitor
- Target
- Proto-oncogene tyrosine-protein kinase receptor Ret
- Protein identifier
- P07949
- Mechanism
- Coiled-coil domain-containing protein 6/Tyrosine-protein kinase receptor RET inhibitor
- Action type
- Inhibitor
- Target
- Coiled-coil domain-containing protein 6/Tyrosine-protein kinase receptor RET
- Mechanism
- Kinesin-1 heavy chain/ Tyrosine-protein kinase receptor RET inhibitor
- Action type
- Inhibitor
- Target
- Kinesin-1 heavy chain/ Tyrosine-protein kinase receptor RET
- Mechanism
- Tyrosine-protein kinase receptor RET inhibitor
- Action type
- Inhibitor
- Target
- Proto-oncogene tyrosine-protein kinase receptor Ret
- Action type
- Inhibitor
- Gene symbol
- RET
- Protein identifier
- P07949
- Organism
- Homo sapiens
- Target development level
- Clinical
- Action type
- Inhibitor
- Gene symbol
- AURKB
- Protein identifier
- Q96GD4
- Organism
- Homo sapiens
- Target development level
- Chemical evidence
- Condition
- Adenocarcinoma, Follicular
- Highest recorded phase
- 2
- Condition identifier
- EFO:0000501
- Subject identifier
- D018263
- Condition
- Neoplasms
- Highest recorded phase
- 4
- Condition identifier
- EFO:0000616
- Subject identifier
- D009369
- Condition
- Thyroid Neoplasms
- Highest recorded phase
- 4
- Condition identifier
- EFO:0000641
- Subject identifier
- D013964
- Condition
- Liver Diseases
- Highest recorded phase
- 1
- Condition identifier
- EFO:0001421
- Subject identifier
- D008107
- Condition
- Carcinoma, Non-Small-Cell Lung
- Highest recorded phase
- 4
- Condition identifier
- EFO:0003060
- Subject identifier
- D002289
- Condition
- Thyroid Neoplasms
- Highest recorded phase
- 4
- Condition identifier
- EFO:0003841
- Subject identifier
- D013964
- Condition
- Renal Insufficiency
- Highest recorded phase
- 1
- Condition identifier
- HP:0000083
- Subject identifier
- D051437
- Condition
- Thyroid Neoplasms
- Highest recorded phase
- 4
- Condition identifier
- MONDO:0002108
- Subject identifier
- D013964
- Condition
- Neoplasms
- Highest recorded phase
- 4
- Condition identifier
- MONDO:0004992
- Subject identifier
- D009369
- Condition
- Carcinoma, Medullary
- Highest recorded phase
- 4
- Condition identifier
- MONDO:0015277
- Subject identifier
- D018276
- Condition identifier
- EFO_0000616
- Condition identifier
- EFO_0000641
- Condition identifier
- EFO_0001421
- Highest recorded phase
- 1
- Condition identifier
- EFO_0003060
- Condition identifier
- EFO_0003841
- Condition identifier
- EFO_0003860
- Condition identifier
- EFO_1000359
- Condition identifier
- EFO_1001950
- Condition identifier
- HP_0000083
- Highest recorded phase
- 1
- Condition identifier
- HP_0002039
- Highest recorded phase
- 1
- Condition identifier
- HP_0004326
- Highest recorded phase
- 1
- Condition identifier
- MONDO_0002108
- Condition identifier
- MONDO_0002108
- Highest recorded phase
- 4
- Condition identifier
- MONDO_0005062
- Highest recorded phase
- 2
- Condition identifier
- MONDO_0005070
- Highest recorded phase
- 4
- Condition identifier
- MONDO_0005075
- Highest recorded phase
- 2
- Condition identifier
- MONDO_0005233
- Highest recorded phase
- 4
- Condition identifier
- MONDO_0006468
- Highest recorded phase
- 2
- Condition identifier
- MONDO_0007254
- Condition identifier
- MONDO_0007254
- Highest recorded phase
- 2
- Condition identifier
- MONDO_0009693
- Highest recorded phase
- 2
- Condition identifier
- MONDO_0015074
- Highest recorded phase
- 4
- Condition identifier
- MONDO_0015075
- Highest recorded phase
- 2
- Condition identifier
- MONDO_0015277
- Condition identifier
- MONDO_0015277
- Highest recorded phase
- 4
And 5 more, listed on the interactive page.
- Event
- blood creatinine increased
- Reports
- 7
- Reporting signal score
- 10.6203
- Event
- febrile infection
- Reports
- 2
- Reporting signal score
- 8.2257
- Event
- inflammatory marker increased
- Reports
- 2
- Reporting signal score
- 6.04018
- Event
- liver function test increased
- Reports
- 4
- Reporting signal score
- 8.07109
- Event
- malignant neoplasm progression
- Reports
- 7
- Reporting signal score
- 11.2554
- Event
- oedema
- Reports
- 5
- Reporting signal score
- 7.28392
- Event
- oedema peripheral
- Reports
- 8
- Reporting signal score
- 8.88929
- Event
- seizure like phenomena
- Reports
- 2
- Reporting signal score
- 8.09638
- Event
- tumour associated fever
- Reports
- 2
- Reporting signal score
- 11.3168
- Event
- urinary tract infection enterococcal
- Reports
- 2
- Reporting signal score
- 8.41858
- NCT02925234
- NCT05159245
- NCT03944772
- NCT04194944
- NCT04268550
- NCT04819100
- NCT05364645
- NCT04211337
- NCT04280081
- NCT05436912
- NCT05469100
- NCT05668962
- Dose
- 120 mg
- Route
- Oral
- How often
- Twice daily
- Do not crush or chew capsules or tablets
- Take with or without food
- Hydrogen bond acceptors
- 10
- Hydrogen bond donors
- 1
- Polar surface area
- 112.04
- Calculated partition coefficient (ALogP)
- 3.28
- Calculated partition coefficient (XLogP)
- 2.5
- Prodrug
- No
- Chirality
- Achiral
- Inorganic
- No
- Rule-of-five violations
- 1
- Rotatable bonds
- 8
- Heavy atoms
- 39
- Molecular formula
- C29H31N7O3
- Monoisotopic mass
- 525.24883788
- Natural product
- No
- 0002-2980
- 0002-3977
- 0002-5340
- 0002-5562
- 0002-6082
- 0002-6120
- Recorded assays
- 260
- Active assays
- 85
Active assay types
- Confirmatory
Related records
Trials (36)
- A Drug Drug Interaction (DDI) Study of Selpercatinib (LY3527723) and Rosuvastatin in Healthy Participants
- A Drug Drug Interaction (DDI) Study of Selpercatinib and Dabigatran in Healthy Participants
- A Relative Bioavailability Study of Selpercatinib (LY3527723) in Healthy Participants
- A Study Comparing Two Formulations of Selpercatinib (LY3527723) in Healthy Participants
- A Study of Absorption, Metabolism, Excretion, and Absolute Bioavailability of Carbon-14-Labelled [14C] Selpercatinib (LY3527723) in Healthy Male Participants
- A Study of Effect of Food and a Proton Pump Inhibitor on Selpercatinib (LY3527723) in Healthy Participants
- A Study of Effect of Selpercatinib (LY3527723) in Participants With Normal and Impaired Renal Function
- A Study of Effect of Selpercatinib (LY3527723) on Corrected QT (QTc) Interval in Healthy Participants
- A Study of Effects of Itraconazole and Rifampin on Selpercatinib (LY3527723) in Healthy Participants
- A Study of Effects of Selpercatinib (LY3527723) on Midazolam in Healthy Participants
- A Study of Effects of Selpercatinib (LY3527723) on Repaglinide in Healthy Participants
- A Study of Effects of Selpercatinib in Hepatically Impaired Participants and Healthy Participants
- A Study of Oral LOXO-292 (Selpercatinib) in Pediatric Participants With Advanced Solid or Primary Central Nervous System (CNS) Tumors
- A Study of Selpercatinib (LOXO-292) in Participants With Advanced Solid Tumors, RET Fusion-Positive Solid Tumors, and Medullary Thyroid Cancer (LIBRETTO-001)
- A Study of Selpercatinib (LY3527723) in Healthy Participants
- A Study of Selpercatinib (LY3527723) in Participants With Advanced or Metastatic RET Fusion-Positive Non-Small Cell Lung Cancer
- A Study of Selpercatinib (LY3527723) in Participants With Advanced Solid Tumors Including RET Fusion-positive Solid Tumors, Medullary Thyroid Cancer and Other Tumors With RET Activation
- A Study of Selpercatinib (LY3527723) in Participants With RET-Mutant Medullary Thyroid Cancer
- A Study of Selpercatinib After Surgery or Radiation in Participants With Non-Small Cell Lung Cancer (NSCLC)
- A Study of the Effect of Food on Selpercatinib (LY3527723) in Healthy Participants
Approved for (7)
- Cancer
- Medullary thyroid gland carcinoma
- Neoplasm
- Non-small cell lung carcinoma
- Thyroid cancer
- Thyroid gland papillary carcinoma
- Thyroid tumor
In development for (3)
- Kidney failure Phase 1
- Liver disorder Phase 1
- Thyroid gland follicular carcinoma Phase 2
Other linked conditions (5)
- Breast cancer
- Colon carcinoma
- Malignant colon neoplasm
- Malignant pancreatic neoplasm
- Pancreatic neoplasm