Bayer to Present New Preclinical and Clinical Data on Advancing Oncology Portfolio

BY Editor

Bayer to Present New preclinical and clinical data on Advancing Oncology Portfolio – Apr 20, 2015– Berlin, Germany (Techreleased) – Bayer HealthCare (Bayer) will present latest preclinical and clinical data on oncolocgy compounds with new mechanism of action including several potent and selective small molecule inhibitors and an antibody-drug conjugate at the American Association for Cancer Research (AACR) 106th Annual Meeting, April 18-22, 2015, in Philadelphia, PA.

The oral presentations include preclinical anti-tumor activity data of BAY 1143572, an oral inhibitor of P-TEFb (positive transcription elongation factor b), which suppresses specific anti-apoptotic and proliferative signals. Bayer will also present new preclinical data on BAY 1238097, a novel bromodomain and extra-terminal (BET) inhibitor with strong anti-tumor activity in hematological tumor models (currently in Phase I), and two Mps1 kinase inhibitors (BAY 1161909 and BAY 1217389), which inactivate the mitotic checkpoint leading to severe chromosome missegregation and tumor cell death (currently in Phase I).

In addition, preclinical data for a selective small molecule pan FGFR1-3 kinase inhibitor (BAY 1163877) and an FGFR2 antibody-drug conjugate (ADC), BAY 1187982, both currently in Phase I clinical development, will be presented. Both investigational agents target fibroblast growth factor receptors (FGFRs), whose increased expression is linked with tumor progression, neoangiogenesis, and chemoresistance. The antibody-drug conjugate carries a microtubule-binding auristatin licensed from Seattle Genetics.

Bayer will also present clinical biomarker analyses of its Phase II development candidate refametinib (BAY 86-9766), an inhibitor of mitogen-activated ERK kinases (MEK), and of its multi-kinase inhibitor regorafenib (Stivarga® ), which is approved for the treatment of metastatic colorectal cancer and gastrointestinal stromal tumors (GIST).

Emerging data from joint projects with external academic and biotech partners will also be presented at AACR: these include new preclinical data presented by the National University of Singapore and/or the National Cancer Center of Singapore on Bayer’s pan CDK inhibitor roniciclib (BAY 1000394, currently in Phase II), the predominant alpha/delta PI3-kinase inhibitor copanlisib (BAY 80-6946, currently in Phase II) and the alpha/beta-balanced PI3-kinase inhibitor, BAY 1082439 (currently in Phase I). In addition, preclinical data from Bayer’s alliance with OncoMed Pharmaceuticals on the two Wnt pathway antagonists, ipafricept and vantictumab, currently in Phase I clinical testing, will be presented. Also, three collaborative Innovative Medicines Initiative (IMI) projects, funded by the unique public-private partnership of the pharmaceutical industry and the European Union, will be highlighted: OncoTrack (genomic cancer diagnostics); Cancer-ID (blood-based biomarker for cancer); and Cancer-PREDECT (in vitro platforms for target validation).

The following list comprises a selection of presentations on Bayer pipeline studies and projects presented at AACR 2015:

Selected Oral Presentations

– BAY 1143572: A first-in-class, highly selective, potent and orally available inhibitor of PTEFb/CDK9 currently in Phase I, inhibits MYC and shows convincing anti-tumor activity in multiple xenograft models by the induction of apoptosis
a) Drug Development Track: Special Session – New Drugs on the Horizon 2; Presentation# DDT02-02
b) Sunday, April 19, 3:45 p.m.-4:10 p.m., Room 204, Pennsylvania Convention Center

– Tumor genotyping in the Phase III GRID study of regorafenib vs placebo in tyrosine kinase inhibitor (TKI)-refractory GIST: Detection of KIT mutations in circulating tumor DNA comparing digital PCR and massive parallel sequencing
a) Minisymposium: Clinical Research: Liquid Biopsies; Presentation# 929
b) Sunday, April 19, 4:05 p.m.-4:20 p.m., Terrace Ballroom I (400 Level), Pennsylvania Convention Center

– Rapid identification of potent and highly selective, oral PTEFb Inhibitor BAY 1143572 with first in class potential
a) Minisymposium: Chemistry: Progress Toward New Drugs and New Drug Technologies; Presentation# 2828
b) Monday, April 20, 3:20 p.m.-3:35 p.m., Room 113, Pennsylvania Convention Center

Selected Poster Presentations

– Anti-tumor efficacy of the selective pan-FGFR Inhibitor BAY 1163877 in preclinical squamous cell carcinoma models of different origin
a) Poster Session: Experimental and Molecular Therapeutics: Tyrosine Kinase and Phosphatase Inhibitors; Abstract# 772
b) Sunday, April 19, 1:00 p.m.-5:00 p.m., Pennsylvania Convention Center, Poster Section 32, Poster# 4

– Pharmacokinetic/pharmacodynamic (PK/PD) and toxicokinetic/toxicodynamic (TK/TD) modeling of preclinical data of FGFR2-ADC (BAY 1187982) to guide dosing in phase I
a) Poster Session: Experimental and Molecular Therapeutics: Growth Factor Receptors and Other Surface Antigens as Targets for Therapy; Abstract# 1683
b) Monday, April 20, 8:00 a.m.-12:00 p.m., Pennsylvania Convention Center, Poster Section 29, Poster# 16

– Preclinical anti-tumor efficacy of FGFR2-ADC BAY 1187982 in patient-derived gastric, breast and ovarian cancer models
a) Poster Session: Experimental and Molecular Therapeutics: Growth Factor Receptors and Other Surface Antigens as Targets for Therapy; Abstract# 1684
b) Monday, April 20, 8:00 a.m.-12:00 p.m., Pennsylvania Convention Center, Poster Section 29, Poster# 17

– Activity of BAY1082439, a balanced PI3K?/? inhibitor, in gastric cancer
a) Poster Session: Experimental and Molecular Therapeutics: PI3K Pathway and Metabolism Modulators; Abstract# 2674
b) Monday, April 20, 1:00 p.m.-5:00 p.m., Pennsylvania Convention Center, Poster Section 32, Poster# 26

– Novel Mps1 kinase inhibitors with potent anti-tumor activity
a) Poster Session: Molecular and Cellular Biology: Targeting Cyclin-Dependent Kinases and Checkpoint Kinases for Cancer Therapy; Abstract# 3090
b) Tuesday, April 21, 8:00 a.m.-12:00 p.m., Pennsylvania Convention Center, Poster Section 9, Poster# 3

– BAY 1238097, a novel BET inhibitor with strong efficacy in hematological tumor models
a) Poster Session: Experimental and Molecular Therapeutics: Epigenetic Targets and BET Inhibitors; Abstract# 3524
b) Tuesday, April 21, 8:00 a.m.-12:00 p.m., Pennsylvania Convention Center, Poster Section 28, Poster# 17

– KRAS wild-type status as detected by circulating tumor DNA analysis may be a prognostic or predictive factor for clinical benefit in patients with unresectable, locally advanced or metastatic pancreatic cancer (PC) treated with the MEK inhibitor refametinib (BAY 86-9766) and gemcitabine
a) Poster Session: Clinical Research: Circulating Free DNA 2; Abstract# 5239
b) Wednesday, April 22, 8:00 a.m.-12:00 p.m., Pennsylvania Convention Center, Poster Section 22, Poster# 10

– Liquid biopsies to prospectively select patients with KRAS or NRAS mutant hepatocellular carcinoma (HCC) in two phase II studies with refametinib
a) Poster Session: Clinical Research: Circulating Free DNA 2; Abstract# 5252
b) Wednesday, April 22, 8:00 a.m.-12:00 p.m., Pennsylvania Convention Center, Poster Section 22, Poster# 23

Further details on additional oral and poster presentations can be found at the AACR website (www.aacr.org).