Difference between revisions of "Masitinib (AB-1010)"

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==Preliminary data==
 
==Preliminary data==
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===[[Gastrointestinal stromal tumor|Gastrointestinal stromal tumor (GIST)]]===
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# Le Cesne A, Blay JY, Bui BN, Bouché O, Adenis A, Domont J, Cioffi A, Ray-Coquard I, Lassau N, Bonvalot S, Moussy A, Kinet JP, Hermine O. Phase II study of oral masitinib mesilate in imatinib-naïve patients with locally advanced or metastatic gastro-intestinal stromal tumour (GIST). Eur J Cancer. 2010 May;46(8):1344-51. Epub 2010 Mar 6. [https://pubmed.ncbi.nlm.nih.gov/20211560/ PubMed]
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# Adenis A, Blay JY, Bui-Nguyen B, Bouché O, Bertucci F, Isambert N, Bompas E, Chaigneau L, Domont J, Ray-Coquard I, Blésius A, Van Tine BA, Bulusu VR, Dubreuil P, Mansfield CD, Acin Y, Moussy A, Hermine O, Le Cesne A. Masitinib in advanced gastrointestinal stromal tumor (GIST) after failure of imatinib: a randomized controlled open-label trial. Ann Oncol. 2014 Sep;25(9):1762-9. Epub 2014 Jul 25. [https://academic.oup.com/annonc/article/25/9/1762/2801236 link to original article] [https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4143095/ link to PMC article] [https://pubmed.ncbi.nlm.nih.gov/25122671/ PubMed]
  
 
===[[Pancreatic cancer]]===
 
===[[Pancreatic cancer]]===
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# Deplanque G, Demarchi M, Hebbar M, Flynn P, Melichar B, Atkins J, Nowara E, Moyé L, Piquemal D, Ritter D, Dubreuil P, Mansfield CD, Acin Y, Moussy A, Hermine O, Hammel P. A randomized, placebo-controlled phase III trial of masitinib plus gemcitabine in the treatment of advanced pancreatic cancer. Ann Oncol. 2015 Apr 9. [Epub ahead of print] [https://www.ncbi.nlm.nih.gov/pubmed/25858497 PubMed]
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# '''AB07012:''' Deplanque G, Demarchi M, Hebbar M, Flynn P, Melichar B, Atkins J, Nowara E, Moyé L, Piquemal D, Ritter D, Dubreuil P, Mansfield CD, Acin Y, Moussy A, Hermine O, Hammel P. A randomized, placebo-controlled phase III trial of masitinib plus gemcitabine in the treatment of advanced pancreatic cancer. Ann Oncol. 2015 Jun;26(6):1194-200. Epub 2015 Apr 9. [https://academic.oup.com/annonc/article/26/6/1194/161899 link to original article] [https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4516046/ link to PMC article] [https://pubmed.ncbi.nlm.nih.gov/25858497/ PubMed]
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# '''AB12005:''' [https://clinicaltrials.gov/study/NCT03766295 NCT03766295]
  
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===[[Sarcoma|Gastrointestinal stromal tumor (GIST)]]===
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===[[Systemic mastocytosis]]===
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# Le Cesne A, Blay JY, Bui BN, Bouché O, Adenis A, Domont J, Cioffi A, Ray-Coquard I, Lassau N, Bonvalot S, Moussy A, Kinet JP, Hermine O. Phase II study of oral masitinib mesilate in imatinib-naïve patients with locally advanced or metastatic gastro-intestinal stromal tumour (GIST). Eur J Cancer. 2010 May;46(8):1344-51. Epub 2010 Mar 6. [https://www.ncbi.nlm.nih.gov/pubmed/20211560 PubMed]
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# '''AB06006:''' Lortholary O, Chandesris MO, Bulai Livideanu C, Paul C, Guillet G, Jassem E, Niedoszytko M, Barete S, Verstovsek S, Grattan C, Damaj G, Canioni D, Fraitag S, Lhermitte L, Georgin Lavialle S, Frenzel L, Afrin LB, Hanssens K, Agopian J, Gaillard R, Kinet JP, Auclair C, Mansfield C, Moussy A, Dubreuil P, Hermine O. Masitinib for treatment of severely symptomatic indolent systemic mastocytosis: a randomised, placebo-controlled, phase 3 study. Lancet. 2017 Feb 11;389(10069):612-620. Epub 2017 Jan 6. [https://doi.org/10.1016/S0140-6736(16)31403-9 link to original article] [https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5985971/ link to PMC article] [https://pubmed.ncbi.nlm.nih.gov/28069279/ PubMed]
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# Adenis A, Blay JY, Bui-Nguyen B, Bouché O, Bertucci F, Isambert N, Bompas E, Chaigneau L, Domont J, Ray-Coquard I, Blésius A, Van Tine BA, Bulusu VR, Dubreuil P, Mansfield CD, Acin Y, Moussy A, Hermine O, Le Cesne A. Masitinib in advanced gastrointestinal stromal tumor (GIST) after failure of imatinib: a randomized controlled open-label trial. Ann Oncol. 2014 Sep;25(9):1762-9. Epub 2014 Jul 25. [https://www.ncbi.nlm.nih.gov/pubmed/25122671 PubMed]
 
  
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[[Category:Drug index]]
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==Also known as==
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[[Category:Chemotherapy]]
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*'''Code name:''' AB-1010
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[[Category:Oral chemotherapy]]
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[[Category:Drugs]]
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[[Category:Oral medications]]
  
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[[Category:Kinase inhibitors]]
 
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[[Category:FAK inhibitors]]
 
 
[[Category:FGFR inhibitors]]
 
[[Category:FGFR inhibitors]]
 
[[Category:KIT inhibitors]]
 
[[Category:KIT inhibitors]]
 
[[Category:PDGFR inhibitors]]
 
[[Category:PDGFR inhibitors]]
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[[Category:PTK2 inhibitors]]
  
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[[Category:Pancreatic cancer medications]]  
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[[Category:Gastrointestinal stromal tumor medications (investigational)]]
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[[Category:Sarcoma medications]]  
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[[Category:Pancreatic cancer medications (investigational)]]  
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[[Category:Systemic mastocytosis medications (investigational)]]
  
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[[Category:Investigational]]
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[[Category:Investigational drugs]]

Latest revision as of 12:26, 27 July 2023

General information

Class/mechanism (from NCI Drug Dictionary): The orally bioavailable mesylate salt of masatinib, a multi-targeted protein tyrosine kinase inhibitor with potential antineoplastic activity. Masitinib selectively binds to and inhibits both the wild-type and mutated forms of the stem cell factor receptor (c-Kit; SCFR); platelet-derived growth factor receptor (PDGFR); fibroblast growth factor receptor 3 (FGFR3); and, to a lesser extent, focal adhesion kinase (FAK).
Route: PO
Extravasation: n/a

Preliminary data

Gastrointestinal stromal tumor (GIST)

  1. Le Cesne A, Blay JY, Bui BN, Bouché O, Adenis A, Domont J, Cioffi A, Ray-Coquard I, Lassau N, Bonvalot S, Moussy A, Kinet JP, Hermine O. Phase II study of oral masitinib mesilate in imatinib-naïve patients with locally advanced or metastatic gastro-intestinal stromal tumour (GIST). Eur J Cancer. 2010 May;46(8):1344-51. Epub 2010 Mar 6. PubMed
  2. Adenis A, Blay JY, Bui-Nguyen B, Bouché O, Bertucci F, Isambert N, Bompas E, Chaigneau L, Domont J, Ray-Coquard I, Blésius A, Van Tine BA, Bulusu VR, Dubreuil P, Mansfield CD, Acin Y, Moussy A, Hermine O, Le Cesne A. Masitinib in advanced gastrointestinal stromal tumor (GIST) after failure of imatinib: a randomized controlled open-label trial. Ann Oncol. 2014 Sep;25(9):1762-9. Epub 2014 Jul 25. link to original article link to PMC article PubMed

Pancreatic cancer

  1. AB07012: Deplanque G, Demarchi M, Hebbar M, Flynn P, Melichar B, Atkins J, Nowara E, Moyé L, Piquemal D, Ritter D, Dubreuil P, Mansfield CD, Acin Y, Moussy A, Hermine O, Hammel P. A randomized, placebo-controlled phase III trial of masitinib plus gemcitabine in the treatment of advanced pancreatic cancer. Ann Oncol. 2015 Jun;26(6):1194-200. Epub 2015 Apr 9. link to original article link to PMC article PubMed
  2. AB12005: NCT03766295

Systemic mastocytosis

  1. AB06006: Lortholary O, Chandesris MO, Bulai Livideanu C, Paul C, Guillet G, Jassem E, Niedoszytko M, Barete S, Verstovsek S, Grattan C, Damaj G, Canioni D, Fraitag S, Lhermitte L, Georgin Lavialle S, Frenzel L, Afrin LB, Hanssens K, Agopian J, Gaillard R, Kinet JP, Auclair C, Mansfield C, Moussy A, Dubreuil P, Hermine O. Masitinib for treatment of severely symptomatic indolent systemic mastocytosis: a randomised, placebo-controlled, phase 3 study. Lancet. 2017 Feb 11;389(10069):612-620. Epub 2017 Jan 6. link to original article link to PMC article PubMed

Also known as

  • Code name: AB-1010
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