| Drug General Information |
| Drug ID |
D0T5DP
|
| Drug Name |
Selumetinib |
|
| Synonyms |
Selumetinib; AZD-6244; ARRY142886; AZD6244; ARRY142886; AZD 6244; AZD-6244; 6UH91I579U; ARRY 142886; ARRY-142886; AZD6244 (Selumetinib); AZD6244(Selumetinib); CHEBI:90227; CHEMBL1614701; MEK inhibitors; Selumetinib (AZD6244); UNII-6UH91I579U |
| Drug Type |
Small molecular drug |
| Company |
AstraZeneca |
| Structure |
|
| Drug Resistance Mutations |
| Target Name |
Dual specificity mitogen-activated protein kinase kinase 1 (MAP2K1) |
Target Info |
| Gene Name |
MAP2K1 |
| Uniprot ID |
MP2K1_HUMAN |
| Species |
Homo sapiens |
| Reference Sequence |
MPKKKPTPIQLNPAPDGSAVNGTSSAETNLEALQKKLEELELDEQQRKRLEAFLTQKQKV
GELKDDDFEKISELGAGNGGVVFKVSHKPSGLVMARKLIHLEIKPAIRNQIIRELQVLHE
CNSPYIVGFYGAFYSDGEISICMEHMDGGSLDQVLKKAGRIPEQILGKVSIAVIKGLTYL
REKHKIMHRDVKPSNILVNSRGEIKLCDFGVSGQLIDSMANSFVGTRSYMSPERLQGTHY
SVQSDIWSMGLSLVEMAVGRYPIPPPDAKELELMFGCQVEGDAAETPPRPRTPGRPLSSY
GMDSRPPMAIFELLDYIVNEPPPKLPSGVFSLEFQDFVNKCLIKNPAERADLKQLMVHAF
IKRSDAEEVDFAGWLCSTIGLNQPSTPTHAAGV [Homo sapiens]
|
| Targeted Disease |
Skin cancer |
| Drug Resistance Mutations |
| Mutation info |
Missense: P124L |
[1] |
|
| Mutation info |
Missense: P124L |
[1], [2], [3] |
|
| Mutation info |
Missense: C121S |
[1], [2], [3] |
| Mutation Frequency |
16% of the patients |
|
| Mutation info |
Missense: K57N |
[1], [2], [3] |
|
| Mutation info |
Missense: P124S |
[1] |
|
| Mutation info |
Missense: G128D |
[1] |
|
| Mutation info |
Missense: F129L |
[1] |
|
| Mutation info |
Missense: D67N |
[1] |
|
| Mutation info |
Missense: E120D |
[1] |
|
| Mutation info |
Missense: F133L |
[1] |
|
| Mutation info |
Missense: H119P |
[1] |
|
| Mutation info |
Missense: I103N |
[1] |
|
| Mutation info |
Missense: I111N |
[1] |
|
| Mutation info |
Missense: I99T |
[1] |
|
| Mutation info |
Missense: K104N |
[1] |
|
| Mutation info |
Missense: L215P |
[1] |
|
| Mutation info |
Missense: Q56P |
[1] |
|
| Mutation info |
Missense: V211D |
[1] |
|
| Mutation info |
Missense: P124L |
[1] |
|
| Mutation info |
Missense: P124L |
[1], [2], [3] |
|
| Mutation info |
Missense: C121S |
[1], [2], [3] |
| Mutation Frequency |
16% of the patients |
|
| Mutation info |
Missense: K57N |
[1], [2], [3] |
|
| Mutation info |
Missense: P124S |
[1] |
|
| Mutation info |
Missense: G128D |
[1] |
|
| Mutation info |
Missense: F129L |
[1] |
|
| Mutation info |
Missense: D67N |
[1] |
|
| Mutation info |
Missense: E120D |
[1] |
|
| Mutation info |
Missense: F133L |
[1] |
|
| Mutation info |
Missense: H119P |
[1] |
|
| Mutation info |
Missense: I103N |
[1] |
|
| Mutation info |
Missense: I111N |
[1] |
|
| Mutation info |
Missense: I99T |
[1] |
|
| Mutation info |
Missense: K104N |
[1] |
|
| Mutation info |
Missense: L215P |
[1] |
|
| Mutation info |
Missense: Q56P |
[1] |
|
| Mutation info |
Missense: V211D |
[1] |
|
| References |
| REF 1 |
MEK1 mutations confer resistance to MEK and B-RAF inhibition. Proc Natl Acad Sci U S A. 2009 Dec 1;106(48):20411-6.
|
| REF 2 |
Dissecting therapeutic resistance to RAF inhibition in melanoma by tumor genomic profiling. J Clin Oncol. 2011 Aug 1;29(22):3085-96.
|
| REF 3 |
Phase II trial of MEK inhibitor selumetinib (AZD6244, ARRY-142886) in patients with BRAFV600E/K-mutated melanoma. Clin Cancer Res. 2013 Apr 15;19(8):2257-64.
|
