Lumakras, Lumykras(sotorasib)
Lumakras, Lumykras (sotorasib) is a small molecule pharmaceutical. Sotorasib was first approved as Lumakras on 2021-05-28. It is used to treat non-small-cell lung carcinoma in the USA. It has been approved in Europe to treat non-small-cell lung carcinoma. It is known to target GTPase KRas.
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Commercial
Therapeutic Areas
Therapeutic Area | MeSH |
|---|---|
| neoplasms | D009369 |
| respiratory tract diseases | D012140 |
Trade Name
FDA
EMA
Lumakras
Labels
FDA
EMA
No data
Indications
FDA
EMA
Indication | Ontology | MeSH | ICD-10 |
|---|---|---|---|
| non-small-cell lung carcinoma | — | D002289 | — |
Agency Specific
FDA
EMA
Expiration | Code | ||
|---|---|---|---|
SOTORASIB, LUMAKRAS, AMGEN INC | |||
| 2028-05-28 | ODE-352 | ||
| 2026-05-28 | NCE | ||
HCPCS
No data
Clinical
Clinical Trials
55 clinical trials
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Indications Phases 4
No data
Indications Phases 3
Indication | MeSH | Ontology | ICD-10 | Ph 1 | Ph 2 | Ph 3 | Ph 4 | Other | Total |
|---|---|---|---|---|---|---|---|---|---|
| Non-small-cell lung carcinoma | D002289 | — | — | 7 | 12 | 1 | — | 1 | 17 |
| Colorectal neoplasms | D015179 | — | — | 1 | 1 | 1 | — | — | 2 |
Indications Phases 2
Indication | MeSH | Ontology | ICD-10 | Ph 1 | Ph 2 | Ph 3 | Ph 4 | Other | Total |
|---|---|---|---|---|---|---|---|---|---|
| Neoplasms | D009369 | — | C80 | 8 | 6 | — | — | — | 9 |
| Lung neoplasms | D008175 | HP_0100526 | C34.90 | — | 3 | — | — | — | 3 |
| Adenocarcinoma of lung | D000077192 | — | — | — | 1 | — | — | — | 1 |
| Pancreatic ductal carcinoma | D021441 | — | — | 1 | 1 | — | — | — | 1 |
| Melanoma | D008545 | — | — | 1 | 1 | — | — | — | 1 |
| Pancreatic neoplasms | D010190 | EFO_0003860 | C25 | 1 | 1 | — | — | — | 1 |
| Mutation | D009154 | — | — | — | 1 | — | — | — | 1 |
Indications Phases 1
Indication | MeSH | Ontology | ICD-10 | Ph 1 | Ph 2 | Ph 3 | Ph 4 | Other | Total |
|---|---|---|---|---|---|---|---|---|---|
| Healthy volunteers/patients | — | — | — | 13 | — | — | — | — | 13 |
| Hepatic insufficiency | D048550 | — | — | 1 | — | — | — | — | 1 |
Indications Without Phase
No data
Epidemiology
Epidemiological information for investigational and approved indications
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Drug
General
| Drug common name | Sotorasib |
| INN | sotorasib |
| Description | Sotorasib is a pyridopyrimidine that is pyrido[2,3-d]pyrimidin-2(1H)-one substituted by 4-methyl-2-(propan-2-yl)pyridin-3-yl, (2S)-2-methyl-4-(prop-2-enoyl)piperazin-1-yl, fluoro and 2-fluoro-6-hydroxyphenyl groups at positions 1, 4, 6 and 7, respectively. It is approved for the treatment of patients with non-small cell lung cancer having KRAS(G12C) mutations. It has a role as an antineoplastic agent. It is a member of acrylamides, a N-acylpiperazine, a pyridopyrimidine, a member of monofluorobenzenes, a member of methylpyridines, a tertiary carboxamide, a tertiary amino compound and a member of phenols. |
| Classification | Small molecule |
| Drug class | Kirsten rat sarcoma (KRAS) inhibitors |
| Image (chem structure or protein) |  |
| Structure (InChI/SMILES or Protein Sequence) | C=CC(=O)N1CCN(c2nc(=O)n(-c3c(C)ccnc3C(C)C)c3nc(-c4c(O)cccc4F)c(F)cc23)[C@@H](C)C1 |
Identifiers
| PDB | — |
| CAS-ID | 2296729-00-3 |
| RxCUI | — |
| ChEMBL ID | CHEMBL4535757 |
| ChEBI ID | — |
| PubChem CID | 137278711 |
| DrugBank | DB15569 |
| UNII ID | 2B2VM6UC8G (ChemIDplus, GSRS) |
Target
Agency Approved
No data
Alternate
KRAS
KRAS
Organism
Homo sapiens
Gene name
KRAS
Gene synonyms
KRAS2, RASK2
NCBI Gene ID
Protein name
GTPase KRas
Protein synonyms
c-K-ras, c-Ki-ras, c-Kirsten-ras protein, cellular c-Ki-ras2 proto-oncogene, cellular transforming proto-oncogene, K-Ras 2, K-ras p21 protein, Ki-Ras, Kirsten rat sarcoma viral oncogene homolog, Kirsten rat sarcoma viral proto-oncogene, KRAS-ENOPH fusion, Kras-Enoph1 fusion protein, oncogene KRAS2, PR310 c-K-ras oncogene, proto-oncogene GTPase, transforming protein p21, v-Ki-ras2 Kirsten rat sarcoma 2 viral oncogene homolog
Uniprot ID
Mouse ortholog
Kras (16653)
GTPase KRas (P32883)
Variants
No data
Financial
No data
Trends
PubMed Central
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Safety
Black-box Warning
No Black-box warning
Adverse Events
Top Adverse Reactions
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156 adverse events reported
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