Literature DB >> 21170669

A phase I/II study of the Src inhibitor saracatinib (AZD0530) in combination with gemcitabine in advanced pancreatic cancer.

Daniel J Renouf1, Malcolm J Moore, David Hedley, Sharlene Gill, Derek Jonker, Eric Chen, David Walde, Rakesh Goel, Bernadette Southwood, Isabelle Gauthier, Wendy Walsh, Lynn McIntosh, Lesley Seymour.   

Abstract

AIM: This phase I/II study of saracatinib in combination with gemcitabine in patients with advanced pancreatic cancer was conducted by the NCIC Clinical Trials Group. The aims were to define the recommended phase II dose (RP2D) of saracatinib when combined with gemcitabine, and assess the efficacy of this combination in advanced pancreatic cancer. PATIENTS AND METHODS: Eligibility criteria included locally advanced or metastatic pancreatic adenocarcinoma and no prior chemotherapy. In phase I saracatinib was escalated in combination with gemcitabine (1000 mg/m(2)) to determine the recommended phase II dose (RP2D). The study was then expanded to a single arm phase II trial using a Simon 2-stage design. The primary endpoint was objective tumor response (OR) plus stable disease ≥ 4 months (SD4) rate; if ≥ 8 patients had OR+SD4, the study would proceed to stage 2.
RESULTS: Thirteen patients were enrolled into the phase I portion of this study. Saracatinib 175 mg PO daily was chosen as the RP2D in combination with gemcitabine. Twenty-one additional patients were then enrolled at the RP2D (phase II). Of the 22 response evaluable patients treated at the RP2D, 9 patients (40.9%) had progressive disease, 6 patients (27.3%) had stable disease for less than 4 months, 5 patients (22.7%) had SD4, and 2 patients (9.1%) had a partial response to treatment. Objective criteria for continuing to stage 2 were thus not met and the trial was closed following the accrual of 34 patients.
CONCLUSION: Saracatinib 175 mg daily in combination with gemcitabine is well tolerated but the combination did not improve efficacy over what would be expected from gemcitabine alone.

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Year:  2010        PMID: 21170669     DOI: 10.1007/s10637-010-9611-3

Source DB:  PubMed          Journal:  Invest New Drugs        ISSN: 0167-6997            Impact factor:   3.850


  19 in total

Review 1.  Alternate endpoints for screening phase II studies.

Authors:  Neesha Dhani; Dongsheng Tu; Daniel J Sargent; Lesley Seymour; Malcolm J Moore
Journal:  Clin Cancer Res       Date:  2009-03-10       Impact factor: 12.531

2.  Optimal two-stage designs for phase II clinical trials.

Authors:  R Simon
Journal:  Control Clin Trials       Date:  1989-03

3.  N-(5-chloro-1,3-benzodioxol-4-yl)-7-[2-(4-methylpiperazin-1-yl)ethoxy]-5- (tetrahydro-2H-pyran-4-yloxy)quinazolin-4-amine, a novel, highly selective, orally available, dual-specific c-Src/Abl kinase inhibitor.

Authors:  Laurent F Hennequin; Jack Allen; Jason Breed; Jon Curwen; Michael Fennell; Tim P Green; Christine Lambert-van der Brempt; Rémy Morgentin; Richard A Norman; Annie Olivier; Ludovic Otterbein; Patrick A Plé; Nicolas Warin; Gerard Costello
Journal:  J Med Chem       Date:  2006-11-02       Impact factor: 7.446

4.  Overexpression and activation of the tyrosine kinase Src in human pancreatic carcinoma.

Authors:  M P Lutz; I B Esser; B B Flossmann-Kast; R Vogelmann; H Lührs; H Friess; M W Büchler; G Adler
Journal:  Biochem Biophys Res Commun       Date:  1998-02-13       Impact factor: 3.575

Review 5.  Chemotherapy and radiotherapy for inoperable advanced pancreatic cancer.

Authors:  D Yip; C Karapetis; A Strickland; C B Steer; D Goldstein
Journal:  Cochrane Database Syst Rev       Date:  2006-07-19

Review 6.  The hunting of the Src.

Authors:  G S Martin
Journal:  Nat Rev Mol Cell Biol       Date:  2001-06       Impact factor: 94.444

7.  Multinomial phase II cancer trials incorporating response and early progression.

Authors:  B Zee; D Melnychuk; J Dancey; E Eisenhauer
Journal:  J Biopharm Stat       Date:  1999-05       Impact factor: 1.051

8.  Src kinase contributes to the metastatic spread of carcinoma cells.

Authors:  Brigitte Boyer; Yveline Bourgeois; Marie-France Poupon
Journal:  Oncogene       Date:  2002-04-04       Impact factor: 9.867

9.  Design of phase II cancer trials using a continuous endpoint of change in tumor size: application to a study of sorafenib and erlotinib in non small-cell lung cancer.

Authors:  Theodore G Karrison; Michael L Maitland; Walter M Stadler; Mark J Ratain
Journal:  J Natl Cancer Inst       Date:  2007-09-25       Impact factor: 13.506

10.  Core signaling pathways in human pancreatic cancers revealed by global genomic analyses.

Authors:  Siân Jones; Xiaosong Zhang; D Williams Parsons; Jimmy Cheng-Ho Lin; Rebecca J Leary; Philipp Angenendt; Parminder Mankoo; Hannah Carter; Hirohiko Kamiyama; Antonio Jimeno; Seung-Mo Hong; Baojin Fu; Ming-Tseh Lin; Eric S Calhoun; Mihoko Kamiyama; Kimberly Walter; Tatiana Nikolskaya; Yuri Nikolsky; James Hartigan; Douglas R Smith; Manuel Hidalgo; Steven D Leach; Alison P Klein; Elizabeth M Jaffee; Michael Goggins; Anirban Maitra; Christine Iacobuzio-Donahue; James R Eshleman; Scott E Kern; Ralph H Hruban; Rachel Karchin; Nickolas Papadopoulos; Giovanni Parmigiani; Bert Vogelstein; Victor E Velculescu; Kenneth W Kinzler
Journal:  Science       Date:  2008-09-04       Impact factor: 47.728

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  23 in total

Review 1.  Overcoming nucleoside analog chemoresistance of pancreatic cancer: a therapeutic challenge.

Authors:  Sau Wai Hung; Hardik R Mody; Rajgopal Govindarajan
Journal:  Cancer Lett       Date:  2012-03-13       Impact factor: 8.679

2.  A phase I study of gemcitabine + dasatinib (gd) or gemcitabine + dasatinib + cetuximab (GDC) in refractory solid tumors.

Authors:  Niharika B Mettu; Donna Niedzwiecki; Christel Rushing; Andrew B Nixon; Jingquan Jia; Sherri Haley; Wanda Honeycutt; Herbert Hurwitz; Johanna C Bendell; Hope Uronis
Journal:  Cancer Chemother Pharmacol       Date:  2019-03-20       Impact factor: 3.333

3.  Inhibition of proto-oncogene c-Src tyrosine kinase: toward a new antiarrhythmic strategy?

Authors:  Luisa Mestroni; Duy Thai Nguyen
Journal:  J Am Coll Cardiol       Date:  2014-01-08       Impact factor: 24.094

4.  Fyn inhibition rescues established memory and synapse loss in Alzheimer mice.

Authors:  Adam C Kaufman; Santiago V Salazar; Laura T Haas; Jinhee Yang; Mikhail A Kostylev; Amanda T Jeng; Sophie A Robinson; Erik C Gunther; Christopher H van Dyck; Haakon B Nygaard; Stephen M Strittmatter
Journal:  Ann Neurol       Date:  2015-03-21       Impact factor: 10.422

5.  Phase II study of saracatinib (AZD0530) in patients with previously treated metastatic colorectal cancer.

Authors:  S M Reddy; S Kopetz; J Morris; N Parikh; W Qiao; M J Overman; D Fogelman; I Shureiqi; C Jacobs; Z Malik; C A Jimenez; R A Wolff; J L Abbruzzese; G Gallick; C Eng
Journal:  Invest New Drugs       Date:  2015-06-12       Impact factor: 3.850

Review 6.  Phase II clinical trials on investigational drugs for the treatment of pancreatic cancers.

Authors:  Edward J Kim; Thomas J Semrad; Richard J Bold
Journal:  Expert Opin Investig Drugs       Date:  2015-03-25       Impact factor: 6.206

Review 7.  Molecular targeted approaches for treatment of pancreatic cancer.

Authors:  Z Q Huang; A K Saluja; V Dudeja; S M Vickers; D J Buchsbaum
Journal:  Curr Pharm Des       Date:  2011       Impact factor: 3.116

Review 8.  Small molecule inhibitors in pancreatic cancer.

Authors:  Jufeng Sun; Cecilia C Russell; Christopher J Scarlett; Adam McCluskey
Journal:  RSC Med Chem       Date:  2020-01-24

Review 9.  Current and future systemic treatment options in metastatic pancreatic cancer.

Authors:  Cagatay Arslan; Suayib Yalcin
Journal:  J Gastrointest Oncol       Date:  2014-08

10.  Identification of initial leads directed at the calmodulin-binding region on the Src-SH2 domain that exhibit anti-proliferation activity against pancreatic cancer.

Authors:  Ywh-Min Tzou; Sarah K Bailey; Kaiyu Yuan; Ronald Shin; Wei Zhang; Yabing Chen; Raj K Singh; Lalita A Shevde; N Rama Krishna
Journal:  Bioorg Med Chem Lett       Date:  2016-01-12       Impact factor: 2.823

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