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A pill that blocked the HER family of growth receptors, tested with capecitabine as second-line treatment for bile duct and gallbladder cancer. It did not beat capecitabine alone in the TreeTopp trial and development stopped.
Varlitinib is an oral reversible inhibitor of EGFR, HER2 and HER4 developed by ASLAN Pharmaceuticals for biliary tract cancer on the rationale that EGFR and HER2 are overexpressed in a quarter to a half of these tumours. The global double-blind TreeTopp phase 2 randomised 127 patients with advanced biliary tract cancer after one gemcitabine-containing line to capecitabine with varlitinib 300 mg twice daily or placebo. Objective response was 9.4 versus 4.8 percent (p 0.42), median progression-free survival 2.83 versus 2.79 months (hazard ratio 0.90) and overall survival 7.8 versus 7.5 months (hazard ratio 1.11); grade 3 or worse adverse events occurred in 66 versus 59 percent. A subgroup analysis suggested a progression-free survival signal in women and in gallbladder cancer (2.9 versus 1.6 months, hazard ratio 0.55, 95 percent confidence interval 0.26 to 1.19), which was hypothesis-generating only. The planned phase 3 part was not pursued and varlitinib is not in development for biliary cancer. It stands as one of several HER-directed small molecules that failed in unselected biliary populations, in contrast to HER2-selected antibody therapy.
ATP-competitive reversible inhibition of EGFR, HER2 and HER4 kinases. Connects to EGFR and HER2.
1.Varlitinib slips into a pocket on EGFR.
Background: ADC sequencing, Antigen escape (antigen loss, lineage switch), BCG-unresponsive, Castration-resistant prostate cancer (CRPC), Circulating tumour DNA (ctDNA). Also on OnCo: Resistance: how tumours escape each drug class · Lines of therapy.
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Query for this drug: (TITLE:"Varlitinib" OR ABSTRACT:"Varlitinib" OR TITLE:"ASLAN001" OR ABSTRACT:"ASLAN001" OR TITLE:"ARRY-334543" OR ABSTRACT:"ARRY-334543") AND (cancer OR tumor OR tumour OR oncology OR carcinoma OR lymphoma OR leukemia OR leukaemia OR myeloma OR sarcoma OR melanoma OR glioma). Results are unfiltered search hits about Varlitinib, not a curated reading list.
Shares Biliary tract cancer (cholangiocarcinoma), Gallbladder cancer and the tag failure.
Shares Biliary tract cancer (cholangiocarcinoma), Gallbladder cancer and the tag failure.
Shares Small-molecule kinase inhibitors and the tag failure.
Shares Small-molecule kinase inhibitors and the tag failure.
Shares Small-molecule kinase inhibitors and the tag failure.
Shares HER2 and the tag failure.
Shares HER2 and the tag failure.
Shares Small-molecule kinase inhibitors and the tag failure.