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INC280*
Phase 2, N/A
c-MET RTK inhibitor
Hemat
INC280 is an oral, selective c-Met RTK inhibitor. Areas of Research: Multiple solid tumors.

Compound DescriptionOral, selective c-Met RTK inhibitor

Areas of ResearchSolid tumors

Proposed Mechanism of ActionINC280 is a highly selective inhibitor of c-MET. In human malignant disease, the c-Met pathway is one of the dysregulated pathways.1 Inappropriate signaling through the c-Met RTK occurs in multiple types of human cancers due to receptor overexpression, gene amplification, gene mutation and/or ligand-dependent activation, and contributes to malignant progression through increased cell proliferation, survival, invasion, and metastasis.1–3 Aberrant c-Met signaling has been documented in many tumor types, including most carcinomas.1–3

Key Preclinical DataINC280 has demonstrated inhibitory activity (IC50 values: 0.2–2 nM) in cell-based biochemical and functional assays that measure c-Met signaling and c-Met–dependent cell proliferation, survival, and migration.3,4 Oral administration of INC280 conferred in vivo activity in blocking both c-Met phosphorylation and tumor growth in mouse tumor models.3,4 Furthermore, INC280 is highly specific for c-Met kinase inhibition.3,5 It has demonstrated > 10,000-fold selectivity to c-Met over a panel of more than 50 human kinases in in vitro assays.3,5

Clinical StatusThere are several ongoing trials of INC280 in various solid tumors. A Phase I, open-label, dose-escalation with expansion to assess the safety and efficacy of INC280 in patients with solid tumors that are refractory to current treatment or for which there is not a current standard of care and whose tumors have dysregulation of the c-MET pathway.

A Phase Ib/II study is assessing the safety and efficacy of escalating doses of INC280 when added to gefitinib in patients with lung cancer that are known to have dysregulation of the c-MET pathway and who have failed after benefiting on a prior treatment with either gefitinib or erlotinib.7 A Phase II study is currently evaluating the safety and efficacy of INC280 in patients with advanced hepatocellular carcinoma known to have dysregulation of the c-MET pathway.8

*INC280 (also known as INCB028060) is licensed from Incyte Corp.
**This is not a comprehensive list of clinical trials for this compound. For additional information please contact your Novartis Medical Representative.
MOA data is based on in vitro/in vivo data. Clinical benefit is unknown.
INC280 is an investigational compound. Efficacy and safety have not been established.
There is no guarantee INC280 will become commercially available.
References
  1. Liu X, Yao W, Newton RC, et al. Targeting the c-Met signaling pathway for cancer therapy. Expert Opin Investig Drugs. 2008;17(7):997–1011.
  2. Birchmeier C, Birchmeier W, Gherardi E, et al. Met, metastasis, motility and more. Nat Rev Mol Cell Biol. 2003;4(12):915–925.
  3. Liu X, Koblish H, Wang Q, et al. Discovery and characterization of INCB028060, a novel, potent and selective Met RTK inhibitor for cancer treatment. In: Proceedings from the 99th Annual Meeting of the American Association for Cancer Research (AACR); April 12–16, 2008; San Diego, CA. Abstract 2577.
  4. Koblish HK, Liu X, Hall L, et al. Preclinical in vivo characterization of INCB028060, a novel, potent and highly selective c-Met inhibitor. In: Proceedings from the 44th Annual Meeting of the American Society of Clinical Oncology (ASCO); May 30–June 3, 2008; Chicago, IL. Abstract 14561.
  5. Liu X. INCB028060, a novel, potent and selective Met RTK inhibitor for cancer treatment. Paper presented at: 4th Annual Summit of the Modern Drug Discovery and Development; October 15–17, 2008; San Diego, CA.
  6. National Institutes of Health (NIH). ClinicalTrials.gov. www.clinicaltrials.gov/ct2/show/NCT01324479. Updated January 21, 2014. Accessed January 27, 2014.
  7. National Institutes of Health (NIH). ClinicalTrials.gov. www.clinicaltrials.gov/ct2/show/NCT01610336. Updated January 21, 2014. Accessed January 27, 2014.
  8. National Institutes of Health (NIH). ClinicalTrials.gov. www.clinicaltrials.gov/ct2/show/NCT01737827. Updated January 15, 2014. Accessed January 19, 2014.
  9. National Institutes of Health (NIH). ClinicalTrials.gov. www.clinicaltrials.gov/ct2/show/NCT01546428. Updated January 16, 2014. Accessed January 27, 2014.
  10. National Institutes of Health (NIH). ClinicalTrials.gov. www.clinicaltrials.gov/ct2/show/NCT01820364. Updated October 29, 2013. Accessed January 13, 2014.
  11. National Institutes of Health (NIH). ClinicalTrials.gov. www.clinicaltrials.gov/ct2/show/NCT01870726. Updated January 16, 2014. Accessed January 19, 2014.
  12. National Institutes of Health (NIH). ClinicalTrials.gov. www.clinicaltrials.gov/ct2/show/NCT01324479. Updated January 21, 2014. Accessed January 27, 2014.
  13. National Institutes of Health (NIH). ClinicalTrials.gov. www.clinicaltrials.gov/ct2/show/NCT01911507. Updated December 10, 2013. Accessed January 16, 2014.

The information contained herein was last updated on April 12, 2013.

All Compounds are either investigational or studied in new indications. Efficacy and safety have not been established. There is no guarantee that they will become commercially available.

The search results, details, and descriptions of clinical trials viewed in this app are supplied by ClinicalTrials.gov and EUtrialregistry.com. This information is maintained by a third party over whom Novartis Pharmaceuticals Corporation has no control. As such, Novartis Pharmaceuticals Corporation does not guarantee the accuracy, completeness, adequacy, or any other aspect of the information contained on this site.