TREETOPP: A phase 2/3 study of varlitinib plus capecitabine versus placebo plus capecitabine as second-line treatment in patients with advanced or metastatic biliary tract cancers (BTCs).
M.M. Javle, D.Y. Oh, M. Ikeda, S. Qin, W.P. Yong, Y. Chao, N. McIntyre, C.Y. Hsieh, L. Chow, A. Chang, M. McHale, B. Lindmark .
ASCO (2018), Abstract Number: TPS4143.

Dose finding study of Varlitinib ± Trastuzumab with Carboplatin/Paclitaxel in advanced solid tumors.
M. Lee, A. Wong, S. Ow, R. Sundar, L.Z. Wang, D.S.P. Tan, R.A. Soo, C.E. Chee, V. Heong, Y.C. Chen, J.S.J. Lim, W.P. Yong, S.E. Lim, B.C. Goh, S.C. Lee.
ASCO (2018), Abstract Number: 2588.

Multicenter open label, randomized Phase 2 trial of varlitinib versus lapatinib in combination with capecitabine in patients with HER2+ metastatic breast cancer (MBC) who failed prior trastuzumab therapy.
S.C. Lee, S.C. Chen, M.S. Dai, G.E. Lee, C.L. Liu, A. Chan, H.K. Chang, L.M. Tseng, W.Y. Chay, L.W.C. Chow, J.L. Peneyra, K.M. Rau, H.C. Wang, A.A. Guancia, M. Head, J.W.Y. Chiu, B. Robinson, M. McHale, A. Barge, B. Lindmark, N. McIntyre, C.Y. Hsieh.
ESMO Asia (2017), Abstract Number 102P.

Initial signals of efficacy in cholangiocarcinoma from a phase Ib trial of varlitinib in combination with doublet chemotherapy (cisplatin + 5-fluororacil or capecitabine).
C.Y. Hsieh, M.S. Wu, M. McHale, B. Lindmark, L. Chow, Y. Chao.
ASCO (2017), Abstract Number e15671.

Pan-HER inhibitor, varlitinib (ASLAN001) disrupts HER/ERK signaling and causes apoptosis in triple negative breast cancer cells.
C.Y. Liu, T.T. Huang, C.T. Huang,  H.P. Yang, L.M. Tseng, C.W. Shiau, K.F. Chen.
AACR (2017), Abstract Number 2087.

Varlitinib to demonstrate anti-tumour efficacy in patient-derived hepatocellular carcinoma xenograft models.
C.Y. Hsieh, L. Ooi, R. Ong, B. Lindmark, M. McHale, H.T. Huynh.
ASCO (2016), Abstract Number e15598.

Varlitinib demonstrates potent antitumour efficacy in patient-derived gastric cancer xenograft models.
H.T. Huynh, R. Ong, B. Lindmark, M. McHale, A.G.L. Ooi.
AACR (2016), Abstract Number 4719.

Phase IIA study to evaluate the biological activity of varlitinib (ASLAN001) in HER-1/2 co-expressing or HER-2 amplified advanced gastric cancer.
J. Kim, S. Im, K. Lee, J.W. Kim, K. Lee, S. Han, T. Kim, I.S. Choi, D. Oh, N. Lee, C. Song, M. Foster, M. McHale, A. Barge, W.H. Kim, Y. Bang
ESMO (2014), Abstract Number 664P.

Pan-ErbB inhibition by varlitinib (ARRY-334543) is superior to selective ErbB inhibition in a preclinical model that signals through multiple ErbB receptors.
R.Blackwell, K. Bouhana, S. Winski, P. Lee, J. Winkler, D. Walker, J. Garrus.
AACR (2010), Abstract Number 3610.

In vivo activity of varlitinib (ARRY-334543), a potent, small molecule inhibitor of EGFR/ErbB-2 in combination with trastuzumab, capecitabine or docetaxel.
D. Anderson, C. Napier, A. Avrutskaya, A. White, T. Pheneger, J. Winkler, P. Lee.
AACR (2009), Abstract Number 1757

Differential activity of varlitinib (ARRY-543), a potent, small molecule inhibitor of EGFR/ErbB2 compared to lapatinib in in vivo xenograft models.
K.Bouhana, T. Pheneger, R. Woessner, G. Tarlton, I.V. Carlowitz, K. Hoffman, E. Wallace, K. Koch, J. Winkler, S. Winski, P. Lee.
AACR (2008). Abstract Number 4848.

In vivo activity of varlitinib (ARRY-334543), a potent, small molecule inhibitor of EGFR/ErbB-2 in combination with trastuzumab or docetaxel.
P.Lee, D. Anderson, A. Avrutskaya, A. White, T. Pheneger, J. Winkler.
CTRC-AACR San Antonio Breast Cancer Symposium (2008). Abstract Number 2150.

In vivo anti-tumour activity of varlitinib (ARRY-334543), a small molecule inhibitor of EGFR and ErbB-2.
T.Pheneger, R. Woessner, S. Winski, D. Anderson, J. Lyssikatos, B. Bernat, G. Miknis, G. Topalov, L. Ren, E. Wallace, P. Lee.
AACR-NCI-EORTC (2005). Abstract Number A247.

Varlitinib (ARRY-334543), a potent, orally active small molecule inhibitor of EGFR and ErbB-2.
G.Miknis, E. Wallace, J. Lyssikatos, P. Lee, Q. Zhao, J. Hans, G. Topalov, A. Buckmelter, G. Tarlton, L. Ren, J. Tullis, B. Bernat, L.P. Opie, I.V. Carlowitz, J. Parry, T. Morales, M. Perrier, R. Woessner, T. Pheneger, K. Hoffman, J. Winkler, K. Koch.
AACR (2005). Abstract Number 3399.

Related Publications

Adaptive Reprogramming of De Novo Pyrimidine Synthesis Is a Metabolic Vulnerability in Triple-Negative Breast Cancer.
K.K. Brown, J.B. Spinelli, J.M. Asara, A. Toker.
Cancer Discovery (2017), 7(4), 1-9.

PTEN regulates glutamine flux to pyrimidine synthesis and sensitivity to dihydroorotate dehydrogenase inhibition.
Mathur, E. Stratikopoulos, S. Ozturk, N. Steinbach, S. Pegno, S. Schoenfeld, R. Yong, V.V. Murty, J.M. Asara, L.C. Cantley, R. Parsons.
Cancer Discovery (2017), 7(4), 380-390.

Inhibition of Dihydroorotate Dehydrogenase Overcomes Differentiation Blockade in Acute Myeloid Leukemia.
D.B. Sykes, Y.S. Kfoury, F.E. Mercier, M.J. Wawer, J.M. Law, M.K. Haynes, T.A. Lewis, A. Schajnovitz, E. Jain, D. Lee, H. Meyer, K.A. Pierce, N.J. Tolliday, A. Waller, S.J. Ferrara, A.L. Eheim, D. Stoeckigt, K.L. Maxcy, J.M. Cobert, J. Bachand, B.A. Szekely, S. Mukherjee, L.A. Sklar, J.D. Kotz, C.B. Clish, R.I. Sadreyev, P.A. Clemons, A. Janzer, S.L. Schreiber, D.T. Scadden.
Cell (2016), 167, 1-16.

The Role of Dihydroorotate Dehydrogenase in Apoptosis Induction in Response to Inhibition of the Mitochondrial Respiratory Chain Complex III.
A.A. Khutornenko, A.A. Dalina, B.V. Chernyak, P.M. Chumakov, A.G. Evstafieva.
Acta Naturae (2014), 6(1), 69-75.

Pyrimidine biosynthesis links mitochondrial respiration to the p53 pathway.
A.A. Khutornenko, V.V. Roudko, B.V. Chernyak, A.B. Vartapetian, P.M. Chumakov, A.G. Evstafieva.
PNAS (2010), 107(29), 12828-12833.

RON kinase: A target for treatment of cancer-induced bone destruction and osteoporosis.
Andrade, J. Fornetti, L. Zhao, S.C. Miller, R.L. Randall, N. Anderson, S.E. Waltz, M. McHale, A.L. Welm.
Science Translational Medicine (2017), 9(374), eaai9338.

Pre-clinical efficacy of RON kinase inhibitors alone and in combination with PI3K inhibitors for treatment of sfRon-expressing breast cancer patient-derived xenografts.
M. Bieniasz, P. Radhakrishnan, N. Faham, J-P. De La O, A. L. Welm.
Clinical Cancer Research (2015), 21 (16); doi: 10.1158/1078-0432.CCR-14-3283  

Inhibition of Ron Kinase Blocks Conversion of Micrometastases to Overt Metastases by Boosting Antitumor Immunity.
H. Eyob, H.A. Ekiz, Y.S. DeRose, S.E. Waltz, M.A. Williams, A.L. Welm
Cancer Discovery 2013, 3, 751-760.

RON promotes the metastatic spread of breast carcinomas by subverting antitumor immune responses.
H. Eyob, H.A. Ekiz, A.L. Welm
Oncoimmunology (2013), 2(9), e25670.

RON’s new role.
C. Cain
SciBX 6(21); doi: 10.1038/scibx.2013.507