Kura Pipeline

Scientific Publications

Kura Presentations and Publications:

Preliminary evidence of clinical activity with tipifarnib in squamous cell carcinomas of the head & neck (SCCHN) with HRAS mutations.   15th International Congress on Targeted Anticancer Therapies (TAT 2017) Presentation
download here

Targeting the RAS-ERK Pathway. 9th European Scientific Oncology Conference (ESOC-9) Presentation
download here

External References:

Protein farnesylation:
Cox, et al. Targeting RAS Membrane Association: Back to the Future for Anti-RAS Drug Discovery? Clin. Cancer Res, 21(8), 1819-1827 (April 2015) 

Berndt, et al. Targeting protein prenylation for cancer therapy. Nature Reviews Cancer 11, 775-791 (November 2011) 

HRAS:
Chen, et al. Transformation by Hras(G12V) is consistently associated with mutant allele copy gains and is reversed by farnesyl transferase inhibition. Oncogene, 33(47):5442-9 (2014 Nov 20) 

PTCL:
Witzig, et al. Multi-institutional phase 2 study of the farnesyltransferase inhibitor tipifarnib (R115777) in patients with relapsed and refractory lymphomas. Blood. 2011 Nov 3; 118(18):4882-9

MDS:
Fenaux, et al. A multicenter phase 2 study of the farnesyltransferase inhibitor tipifarnib in intermediate- to high-risk myelodysplastic syndrome. Blood. 2007 May 15; 109(10):4158-63

CMML:

Fenaux, et al. A multicenter phase 2 study of the farnesyltransferase inhibitor tipifarnib in intermediate- to high-risk myelodysplastic syndrome. Blood. 2007 May 15; 109(10):4158-63

KO-947 / ERK
Kura Presentations and Publications:
KO-947, a Potent and Selective ERK Inhibitor with Slow Dissociation Kinetics. EORTC 2016 Poster download here
Targeting the RAS-ERK Pathway. 9th European Scientific Oncology Conference (ESOC-9) Presentation download here

External References:
Samatar and Poulikakos. Targeting RAS–ERK signalling in cancer: promises and challenges. Nature Reviews Drug Discovery 13, 928–942 (2014)

Menin-MLL
Kura Presentations and Publications:
Discovery of novel menin-MLL small molecule inhibitors that display high potency and selectivity in vitro and in vivo. EORTC 2016 Poster download here

External References:
Borkin, et al. Pharmacologic inhibition of the Menin-MLL interaction blocks progression of MLL leukemia in vivo. Cancer Cell. 2015 Apr 13;27 (4):589-602