A Phase 1/2 Study of TPX-0131, A Novel Oral ALK Tyrosine Kinase Inhibitor in Subjects with ALK+ Advanced or Metastatic NSCLC

Protocol # :
Non Small Cell Lung Cancer
Non-Small Cell Lung Cancer
Advanced Solid Tumor
Metastatic Solid Tumor
ALK Gene Mutation
Disease Sites
Principal Investigator
Lin, Jessica
Site Research Nurses
Janell, Samantha
Kelley, Elaine
Lam, Ethan
Souza, Joseph
Sullivan, Molly, O'Brien

Trial Description

A phase 1, first-in-human, open-label study to evaluate the safety, tolerability, PK, and
efficacy of the novel ALK inhibitor TPX-0131 in pretreated subjects with ALK+ advanced or
metastatic non-small cell lung cancer (NSCLC).

Eligibility Requirements

Inclusion Criteria:

- Age ≥ 18 (or as required by local regulation).

- Histological or cytological confirmation of advanced/metastatic ALK+ NSCLC.

- Pretreated with up to three prior lines of an ALK TKI treatment, including at least
one prior line of a second or third-generation ALK TKI (alectinib, brigatinib,
ensartinib, or lorlatinib) in Phase 1.

- ECOG performance status ≤ 1.

- Existence of measurable or evaluable disease (according to Response evaluation
criteria in solid tumors [RECIST v1.1] criteria).

- Subjects with asymptomatic CNS metastases and/or asymptomatic leptomeningeal
carcinomatosis are eligible.

- Adequate organ function.

Exclusion Criteria:

- Major surgery within four weeks of the start of TPX-0131 treatment.

- Clinically significant cardiovascular disease

- Any of the following cardiac criteria:

- Mean resting corrected QT interval (QTc) > 470 msec obtained from three ECGs and
any factors that increase the risk of QTc prolongation or arrhythmic events

- Any clinically important abnormalities in rhythm, conduction, or morphology of
resting ECG

- Known clinically significant active infections not controlled with systemic treatment
(bacterial, fungal, viral including HIV positivity).

- Gastrointestinal disease or other malabsorption syndromes that would impact drug

- Subjects being treated with or anticipating the need for treatment with strong CYP3A4
inhibitors or inducers.

- Subjects with current or anticipated need for drugs that are sensitive CYP2C9
substrates with narrow therapeutic indices.