This is an open-label, phase 1/1b study evaluating the safety, tolerability, pharmacokinetic (what the body does to the drug), pharmacodynamic (what the drug does to the body), and antitumor activity of CGT4255 in adult participants with advanced solid tumors with ERBB2 alterations or HER2 overexpression.
Part A: Locally advanced, metastatic, and/or unresectable solid tumor with documented ERBB2-activating alteration or NRG1 gene fusion in blood and/or tumor or HER2 overexpression in tumor
Part B: Locally advanced, metastatic, and/or unresectable NSCLC with documented ERBB2 mutation in blood and/or tumor
Part C: Locally advanced, metastatic and/or unresectable breast cancer with documented ERBB2 mutation in blood and/or tumor or HER overexpression in tumor
Have measurable disease per RECIST v1.1.
Received small molecule chemotherapy or anticancer therapies or radiotherapy within certain timeframes before first dose of study drug.
Major surgeries (eg, craniotomy and thoracotomy) within 4 weeks of the first dose of study drug.
Treatment with palliative focal radiotherapy (cranial or extracranial) (eg, stereotactic radiosurgery or intensity-modulated radiation therapy) ≤2 weeks before the first dose of study drug; treatment with whole-brain radiotherapy ≤4 weeks before the first dose of study drug.
Clinically significant cardiac disease.
Sequential
CGT4255
DrugCGT4255 Daily Oral Administration
Incidence and grade of Adverse Events (AEs) and Serious Adverse Events (SAEs) [Part A]
1\. Incidence and grade of Adverse Events (AEs) and Serious Adverse Events (SAEs) and AEs leading to dose modifications and dose limiting toxicities (DLTs) to determine the maximum tolerated dose (MTD) or the maximum evaluated dose (MED) in participants with ERBB2-altered advanced solid tumors
Overall Response Rate [Part B and Part C]
Overall Response Rate (ORR), determined by confirmed CR + PR of all lesions (intracranial and extracranial), based on Investigator assessment using the whole-body RECIST v1.1 in participants with ERBB2-mutated NSCLC with Brain Metastases (BM) and in participants with ERBB2-mutated or HER2-positive breast cancer with BM ± leptomeningeal disease (LMD)
Incidence and grade of Adverse Events (AEs) and Serious Adverse Events (SAEs) [Part B and C]
Incidence and grade of Adverse Events (AEs), Serious Adverse Events (SAEs) and AEs leading to dose modification in participants with ERBB2-mutated NSCLC with Brain Metastases (BM) and in participants with ERBB2-mutated or HER2-positive breast cancer with BM ± leptomeningeal disease (LMD)
Pharmacokinetics [Part A]
Area under the concentration-time curve (AUC) in participants with ERBB2 altered advanced solid tumors
Pharmacokinetics [Part A]
Maximum observed concentration (Cmax) in participants with ERBB2 altered advanced solid tumors
Pharmacokinetics [Part A]
Observed concentration at pre-dose (Ctrough)
Click on the lead sponsor to view all of their trials.
