Difference between revisions of "Barasertib (AZD-1152)"
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| − | =Mechanism of action= | + | ==Mechanism of action== |
| − | Aurora B kinase | + | From the [https://www.cancer.gov/publications/dictionaries/cancer-drug?cdrid=496937 NCI Drug Dictionary]: An orally bioavailable, small-molecule, dihydrogen phosphate prodrug of the pyrazoloquinazoline Aurora kinase inhibitor AZD1152–hydroxyquinazoline pyrazol anilide (AZD1152-HQPA) with potential antineoplastic activity. Upon administration and rapid conversion from the prodrug form in plasma, barasertib specifically binds to and inhibits Aurora kinase B, which results in the disruption of spindle checkpoint functions and chromosome alignment and, so, the disruption of chromosome segregation and cytokinesis. Consequently, cell division and cell proliferation are inhibited and apoptosis is induced in Aurora kinase B-overexpressing tumor cells. |
| − | =Preliminary data= | + | ==Preliminary data== |
| − | ==[[Acute myeloid leukemia]]== | + | ===[[Acute myeloid leukemia]]=== |
| − | # Löwenberg B, Muus P, Ossenkoppele G, Rousselot P, Cahn JY, Ifrah N, Martinelli G, Amadori S, Berman E, Sonneveld P, Jongen-Lavrencic M, Rigaudeau S, Stockman P, Goudie A, Faderl S, Jabbour E, Kantarjian H. Phase 1/2 study to assess the safety, efficacy, and pharmacokinetics of barasertib (AZD1152) in patients with advanced acute myeloid leukemia. Blood. 2011 Dec 1;118(23):6030-6. Epub 2011 Oct 5. [https://www.ncbi.nlm.nih.gov/pubmed/21976672 PubMed] | + | # '''D1531C00007:''' Löwenberg B, Muus P, Ossenkoppele G, Rousselot P, Cahn JY, Ifrah N, Martinelli G, Amadori S, Berman E, Sonneveld P, Jongen-Lavrencic M, Rigaudeau S, Stockman P, Goudie A, Faderl S, Jabbour E, Kantarjian H. Phase 1/2 study to assess the safety, efficacy, and pharmacokinetics of barasertib (AZD1152) in patients with advanced acute myeloid leukemia. Blood. 2011 Dec 1;118(23):6030-6. Epub 2011 Oct 5. [https://doi.org/10.1182/blood-2011-07-366930 link to original article] [https://www.ncbi.nlm.nih.gov/pmc/articles/pmc4186639/ link to PMC article] [https://pubmed.ncbi.nlm.nih.gov/21976672/ PubMed] [https://clinicaltrials.gov/study/NCT00497991 NCT00497991] |
| − | # Kantarjian HM, Martinelli G, Jabbour EJ, Quintás-Cardama A, Ando K, Bay JO, Wei A, Gröpper S, Papayannidis C, Owen K, Pike L, Schmitt N, Stockman PK, Giagounidis A; SPARK-AML1 Investigators. Stage I of a phase 2 study assessing the efficacy, safety, and tolerability of barasertib (AZD1152) versus low-dose cytosine arabinoside in elderly patients with acute myeloid leukemia. Cancer. 2013 Jul 15;119(14):2611-9. Epub 2013 Apr 19. [https://www.ncbi.nlm.nih.gov/pubmed/23605952 PubMed] | + | # '''SPARK-AML1:''' Kantarjian HM, Martinelli G, Jabbour EJ, Quintás-Cardama A, Ando K, Bay JO, Wei A, Gröpper S, Papayannidis C, Owen K, Pike L, Schmitt N, Stockman PK, Giagounidis A; SPARK-AML1 Investigators. Stage I of a phase 2 study assessing the efficacy, safety, and tolerability of barasertib (AZD1152) versus low-dose cytosine arabinoside in elderly patients with acute myeloid leukemia. Cancer. 2013 Jul 15;119(14):2611-9. Epub 2013 Apr 19. [https://doi.org/10.1002/cncr.28113 link to original article] [https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4132839/ link to PMC article] [https://pubmed.ncbi.nlm.nih.gov/23605952/ PubMed] [https://clinicaltrials.gov/study/NCT00952588 NCT00952588] |
| + | |||
| + | ==Also known as== | ||
| + | *'''Code name:''' AZD-1152 | ||
| + | |||
| + | [[Category:Drugs]] | ||
| + | [[Category:Oral medications]] | ||
| − | |||
| − | |||
| − | |||
[[Category:Aurora kinase inhibitors]] | [[Category:Aurora kinase inhibitors]] | ||
| − | [[Category:Acute myeloid leukemia medications]] | + | [[Category:Acute myeloid leukemia medications (investigational)]] |
| − | [[Category:Investigational]] | + | [[Category:Investigational drugs]] |
Latest revision as of 10:57, 6 July 2024
Mechanism of action
From the NCI Drug Dictionary: An orally bioavailable, small-molecule, dihydrogen phosphate prodrug of the pyrazoloquinazoline Aurora kinase inhibitor AZD1152–hydroxyquinazoline pyrazol anilide (AZD1152-HQPA) with potential antineoplastic activity. Upon administration and rapid conversion from the prodrug form in plasma, barasertib specifically binds to and inhibits Aurora kinase B, which results in the disruption of spindle checkpoint functions and chromosome alignment and, so, the disruption of chromosome segregation and cytokinesis. Consequently, cell division and cell proliferation are inhibited and apoptosis is induced in Aurora kinase B-overexpressing tumor cells.
Preliminary data
Acute myeloid leukemia
- D1531C00007: Löwenberg B, Muus P, Ossenkoppele G, Rousselot P, Cahn JY, Ifrah N, Martinelli G, Amadori S, Berman E, Sonneveld P, Jongen-Lavrencic M, Rigaudeau S, Stockman P, Goudie A, Faderl S, Jabbour E, Kantarjian H. Phase 1/2 study to assess the safety, efficacy, and pharmacokinetics of barasertib (AZD1152) in patients with advanced acute myeloid leukemia. Blood. 2011 Dec 1;118(23):6030-6. Epub 2011 Oct 5. link to original article link to PMC article PubMed NCT00497991
- SPARK-AML1: Kantarjian HM, Martinelli G, Jabbour EJ, Quintás-Cardama A, Ando K, Bay JO, Wei A, Gröpper S, Papayannidis C, Owen K, Pike L, Schmitt N, Stockman PK, Giagounidis A; SPARK-AML1 Investigators. Stage I of a phase 2 study assessing the efficacy, safety, and tolerability of barasertib (AZD1152) versus low-dose cytosine arabinoside in elderly patients with acute myeloid leukemia. Cancer. 2013 Jul 15;119(14):2611-9. Epub 2013 Apr 19. link to original article link to PMC article PubMed NCT00952588
Also known as
- Code name: AZD-1152