Details
Stereochemistry | ABSOLUTE |
Molecular Formula | C15H15FIN3O3.ClH |
Molecular Weight | 467.662 |
Optical Activity | UNSPECIFIED |
Defined Stereocenters | 1 / 1 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
Cl.OC[C@@H](O)CNC(=O)C1=C(NC2=C(F)C=C(I)C=C2)C=NC=C1
InChI
InChIKey=HIEXZUXKTABHCP-PPHPATTJSA-N
InChI=1S/C15H15FIN3O3.ClH/c16-12-5-9(17)1-2-13(12)20-14-7-18-4-3-11(14)15(23)19-6-10(22)8-21;/h1-5,7,10,20-22H,6,8H2,(H,19,23);1H/t10-;/m0./s1
DescriptionSources: https://www.ncbi.nlm.nih.gov/pubmed/20331454Curator's Comment: description was created based on several sources, including
http://ar2014.merckgroup.com/management-report/fundamental-information-about-the-group/research-and-development-at-merck
Sources: https://www.ncbi.nlm.nih.gov/pubmed/20331454
Curator's Comment: description was created based on several sources, including
http://ar2014.merckgroup.com/management-report/fundamental-information-about-the-group/research-and-development-at-merck
Pimasertib) (N-[(2S)-2,3-dihydroxypropyl]-3-[(2-fluoro-4-iodophenyl)amino]isonicotinamide hydrochloride; AS703026), a highly selective, potent, ATP non-competitive allosteric inhibitor of MEK1/2. It binds to MEK1/2 in an allosteric site that is distinct from, yet in close proximity to, the ATP binding site. Binding to this allosteric site prevents the activation of MEK1/2. Pimasertib continues to be investigated in patients with NRAS mutant malignant melanoma in a Phase II trial. This drug was discontinued in a combination with SAR245409 for Phase II study in low-grade serous ovarian cancer. This decision was based on the results of a futility analysis, conducted by the IDMC, which indicated that the trial was no longer expected to achieve its objective of showing a meaningful difference between the efficacies of the combination compared with pimasertib alone. The further development of pimasertib in pancreatic cancer was also discontinued, as a Phase II study in this indication did not reach its primary endpoint of prolongation of progression-free survival
Originator
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
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Target ID: CHEMBL2111289 Sources: https://www.ncbi.nlm.nih.gov/pubmed/20331454 |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
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Primary | Unknown Approved UseUnknown |
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Primary | Unknown Approved UseUnknown |
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Primary | Unknown Approved UseUnknown |
Sample Use Guides
Pimasertib will be administered as oral capsule at a dose of 60 mg twice daily continuously. Treatment will consist of repeated 21-day cycles which will be continued until progression of the disease, unacceptable toxicity, withdrawal of informed consent, or death, whichever comes first.
Route of Administration:
Oral
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/21118963
AS703026 (PIMASERTIB) (10 μM) effectively inhibits the ERK pathway, proliferation, and transformation in human DLD-1 colorectal cancer cells what carry a mutant allele of K-Ras (D-MUT).
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Classification Tree | Code System | Code | ||
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FDA ORPHAN DRUG |
297909
Created by
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FDA ORPHAN DRUG |
328110
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EU-Orphan Drug |
EU/3/10/824
Created by
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52918382
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PRIMARY | |||
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EU/3/09/685(POSITIVE)
Created by
admin on Sat Dec 16 02:07:57 GMT 2023 , Edited by admin on Sat Dec 16 02:07:57 GMT 2023
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PRIMARY | Treatment of pancreatic cancer 8/10/2009 Positive | ||
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EU/3/10/824 (POSITIVE)
Created by
admin on Sat Dec 16 02:07:57 GMT 2023 , Edited by admin on Sat Dec 16 02:07:57 GMT 2023
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PRIMARY | Treatment of acute myeloid leukaemia 17/12/2010 Positive | ||
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DTXSID60154058
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PRIMARY | |||
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ZZ-117
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1236361-78-6
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100000155425
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SUB129490
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C166935
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6GS1ULF5HV
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ACTIVE MOIETY
SUBSTANCE RECORD