A Study of TAS2940 in Participants With Locally Advanced or Metastatic Solid Tumor Cancer

A Phase 1 Study of TAS2940 in Patients With Locally Advanced or Metastatic Solid Tumors With EGFR and / or HER2 Aberrations

This is a first-in-human, open label, multicenter study to assess the safety, tolerability, pharmacokinetics, pharmacodynamics, and the preliminary antitumor activity of TAS2940 in patients with advanced or metastatic solid tumors who are not candidates for approved or available therapies.

TAS2940 is a small molecule inhibitor of ERBB family proteins HER2 and EGFR. It has not been evaluated in human subjects yet. The study will be conducted in 2 parts, dose escalation and dose expansion. The dose escalation part will assess the safety and determine the maximum tolerated dose, the recommended phase 2 dose and the recommended dosing regimen of TAS2940 administered orally. The dose expansion part will assess preliminary anti-tumor activity in select solid tumors characterized by HER2 or EGFR aberrations.

Inclusion Criteria:

• Have histologically confirmed solid cancer that is locally advanced and metastatic and available standard treatment options have been exhausted
• Have adequate organ function
• ECOG PS 0-1

Dose Escalation:

• Have measurable or non- measurable disease per RECIST criteria v1.1 or RANO
• Any solid tumor with EGFR and / or HER2 aberration

Dose Expansion:

• Have measurable disease per RECIST criteria v1.1 for solid tumor (excluding primary brain tumor) or RANO (for glioblastoma)
• Cohort A: Non-small cell lung cancer (NSCLC)
• Cohort B: HER2 positive breast cancer
• Cohort C: Recurrent or refractory glioblastoma
• Cohort D: Other solid tumors with EGFR or HER2 aberrations

Exclusion Criteria:

• Non-stable brain metastases
• Have significant cardiovascular disorder
• Have not recovered from prior cancer treatment
• A serious illness or medical condition