A Study of SIGX1094R in Patients With Advanced Solid Tumors

NCT06739291 | Recruiting Phase 1

• 1 other identifier: SG-SIGX1094R-CT-001
• Study Type: interventional
• Target: 102
• Locations: 1 country
• Sites: 1

Brief Summary

This is a phase I clinical, first-in-human study of SIGX1094R monotherapy. The goal of this trial is to evaluate the safety, tolerability, pharmacokinetics (PK), pharmacodynamics (PD), anti-tumor activity and food effect of SIGX1094R in patients with advanced solid tumors.

Conditions

Advanced Solid Tumors

Keywords

Focal Adhesion Kinase inhibitor; FAK inhibitor; SIGX1094R

Outcome Measures

Primary Outcomes (10)

• Incidence of adverse events (AEs)

  To evaluate the safety and tolerability of SIGX1094R. AEs will be evaluated per the National Cancer Institute Common Terminology Criteria for Adverse Events (NCI CTCAE),Version 5.0.

  From the first dose to 28 days after the last dose. Last for approximately 18 months.

• Incidence of serious adverse events (SAEs)

  To evaluate the safety and tolerability of SIGX1094R. SAEs will be evaluated per the National Cancer Institute Common Terminology Criteria for Adverse Events (NCI CTCAE),Version 5.0.

  From the first dose to 28 days after the last dose. Last for approximately 18 months.

• Abnormalities or changes in laboratory tests

  To evaluate the safety and tolerability of SIGX1094R.

  Approximately 18 months

• Abnormalities or changes in vital signs

  To evaluate the safety and tolerability of SIGX1094R.

  Approximately 18 months

• Abnormalities or changes in electrocardiograms (ECGs)

  To evaluate the safety and tolerability of SIGX1094R.

  Approximately 18 months

• Abnormalities or changes in physical examinations

  To evaluate the safety and tolerability of SIGX1094R.

  Approximately 18 months

• Abnormalities or changes in Eastern Oncology Collaborative Group (ECOG) scores

  To evaluate the safety and tolerability of SIGX1094R.

  Approximately 18 months

• Incidence of dose-limiting toxicity (DLT) events

  Collect the incidence, classification, severity, and frequency of DLT. To evaluate the safety and tolerability of SIGX1094R.

  From the first treatment of single dosing (5 days in single dosing period ) to the end of Cycle 1 (21 days a Cycle in multiple dosing period ).

• Maximum tolerated dose (MTD)

  To determine the MTD of SIGX1094R.

  Approximately 18 months

• Recommended phase 2 dose (RP2D)

  To determine the RP2D of SIGX1094R.

  Approximately 18 months

Secondary Outcomes (11)

• Maximum observed concentration (Cmax)

  Time points at Day 1 to Day 5 in single-dose period. Time points at Cycle 1 Day1, Cycle 1 Day 8, Cycle 1 Day15, Cycle 1 Day 21 in Cycle 1, and Cycle n Day 1 from Cycle 2, in multiple-dose period. Each Cycle is 21 days.

• Time of maximum observed concentration (Tmax)

  Time points at Day 1 to Day 5 in single-dose period. Time points at Cycle 1 Day1, Cycle 1 Day 8, Cycle 1 Day15, Cycle 1 Day 21 in Cycle 1, and Cycle n Day 1 from Cycle 2, in multiple-dose period. Each Cycle is 21 days.

• Area under the concentration-time curve (AUC)

  Time points at Day 1 to Day 5 in single-dose period. Time points at Cycle 1 Day1, Cycle 1 Day 8, Cycle 1 Day15, Cycle 1 Day 21 in Cycle 1, and Cycle n Day 1 from Cycle 2, in multiple-dose period. Each Cycle is 21 days.

• Half-life (t1/2)

  Time points at Day 1 to Day 5 in single-dose period. Time points at Cycle 1 Day1, Cycle 1 Day 8, Cycle 1 Day15, Cycle 1 Day 21 in Cycle 1, and Cycle n Day 1 from Cycle 2, in multiple-dose period. Each Cycle is 21 days.

• Objective response rate (ORR)

  Approximately 18 months

Other Outcomes (1)

• 22. Changes of circulating tumor DNA (ctDNA)

  Baseline to approximately 18 months

Study Arms (1)

SIGX1094R

EXPERIMENTAL

Oral SIGX1094R administered once daily.

Drug: SIGX1094R

Interventions

SIGX1094R DRUG

Single drug treatment by SIGX1094R, orally administered once daily.

SIGX1094R

Eligibility Criteria

• Age: 18 Years+
• Sex: all
• Healthy Volunteers: No
• Age Groups: Adult (18-64), Older Adult (65+)

You may qualify if:

• Patients must meet all of the following criteria before being enrolled in the study.
• Patients must be able to understand the procedures and methods of this clinical study, voluntarily participate in the study and sign the ICF.
• Patients aged ≥18 years when signing the ICF, male or female.
• Patients with histologically, cytologically, or clinically proven advanced solid tumors (locally advanced or metastatic) that do not have standard treatment available, have disease progression on/after standard treatment, or cannot tolerate standard treatment.
• Patients with at least one evaluable tumor lesion according to the RECIST v1.1; patients who have no measurable lesions but have evaluable lesions are allowed to be enrolled as judged by the investigator.
• Patients (according to patients' option) will provide a pre-treatment tumor specimen (archival or fresh biopsy samples). If a fresh biopsy is required, procedures more invasive than a core biopsy or significant risk procedures for which the procedure-associated absolute risk of mortality or major morbidity in the patient's clinical setting and specific institution is 2% or higher, should not be utilized. The tumor tissue is used for pFAK status confirmation, without restriction on enrollment.
• ECOG score ≤ 1.
• Life expectancy ≥ 3 months
• Patients with adequate organ function, including:
• Liver function (no history of liver protection therapy 7 days before screening): total bilirubin (TBIL) ≤ 1.5×ULN, alanine aminotransferase (ALT)
• ×ULN, aspartate aminotransferase (AST) ≤ 3×ULN (no liver metastasis); if there is liver metastasis, ALT and AST ≤ 5×ULN; albumin ≥ 30 g/L.
• Renal function: Creatinine clearance ≥ 50 mL/min (calculated according to Cockcroft-Gault formula).
• Hematology (no blood transfusion or hematopoietic stimulating factor treatment within 14 days; no treatment with erythropoietin or thrombopoietin within 7 days): absolute neutrophil count (ANC) ≥ 1.5×10\^9/L, platelet (PLT) ≥ 100×10\^9/L, and hemoglobin (Hb) ≥ 90 g/L.
• Coagulation function: activated partial thromboplastin time ≤ 1.5 × ULN and international normalized ratio ≤ 1.5 × ULN.
• Women of reproductive age must have a negative blood pregnancy test result within 7 days prior to the first dose and promise to adhere to fully effective contraception or abstinence from the beginning of the screening period until 6 months after the last dose of study treatment; male patients must promise to adhere to fully effective contraception or abstinence from the beginning of the screening period until 6 months after the last dose of study treatment.

You may not qualify if:

• Patients who meet any of the following criteria cannot be enrolled in this study.
• Patients with hypersensitivity to the active ingredient or excipient ingredient of SIGX1094R, or a history of severe allergy.
• Having a history of a second primary malignant tumor, excluding cervical carcinoma in situ, cutaneous squamous cell carcinoma, or basal cell carcinoma that has been cured or stabilized as assessed by the investigator;
• Patients who have received cytotoxic chemotherapeutic drugs or small molecule targeted drugs within 4 weeks prior to the first dose. Note: For mitomycin C or nitrosoureas, 6-week washout is required; for small-molecule targeted drugs and oral fluorouracil drugs, a washout period of 2 weeks or 5 T1/2 of the drug (whichever is shorter) is required.
• Anti-tumor endocrine therapy, radiotherapy, interventional embolization, radiofrequency, proton therapy, radioimmunotherapy, immunotherapy or other biotherapies within 4 weeks prior to the first dose (if 5 T1/2 of the drug/therapy used by the patient is confirmed to be \< 4 weeks, 5 T1/2 shall prevail).
• Patients who have received anti-tumor treatment with medicine/proprietary medicine within 2 weeks prior to the first dose. Note: This criterion is relevant to China study only.
• Patients who have received other clinical investigational drugs or therapies that are not on the market within 4 weeks or 5 T1/2 prior to the first dose, whichever is longer.
• Prior treatment with focal adhesion kinase (FAK) inhibitors.
• Patients who have received strong cytochrome P450(CYP)3A4, CYP3A5 inhibitors, or strong CYP3A4 or CYP3A5 inducers, or strong P-gp and BCRP inhibitors, within 14 days prior to the first dose; or cannot stop using such drugs during the study.
• Patients who have received an anti-acid drug or gastric acid reducing agents within 14 days prior to the first dose and cannot be discontinued for the duration of the study. Allow enrollment if administration interval between antacids/gastric acid inhibitors and the study drug is no less than 2 hours during the study period.
• Pregnant or lactating women.
• Patients whose adverse reactions of prior anti-tumor therapy assessed according to CTCAE v5.0 at the time of screening have not returned to Grade ≤ 1 (except for toxicities that are of no safety risk as judged by the investigator, such as alopecia, gasping, γ-glutamyl transferase (GGT) increased, Alkaline phosphatase (ALP) increased, grade 2 peripheral neurotoxicity, and decreased thyroid function stabilized by hormone replacement therapy).
• Presence of clinically symptomatic metastases to central nervous system or meninges or other evidence showing that metastatic lesions in central nervous system or meninges have not yet been controlled at screening, which, at the investigator's discretion, is not suitable for enrollment. Note: Patients with central nervous system or meningeal metastases who are asymptomatic or stable after treatment prior to the first dose may be considered for enrollment.
• A history of severe neurological or psychiatric disorders, including epilepsy, dementia, and moderate to severe depression.
• History of drug abuse or dependence.

Sponsors & Collaborators

• Signet Therapeutics: lead

Study Sites (1)

Beijing Cancer Hospital

Beijing, China

RECRUITING

Central Study Contacts

Signet Therapeutics

CONTACT

0086 0755-82571742; yufang.chen@signettx.com

Study Design

• Study Type: interventional
• Phase: phase 1
• Allocation: NA
• Masking: NONE
• Purpose: TREATMENT
• Intervention Model: SINGLE GROUP
• Sponsor Type: INDUSTRY
• Responsible Party: SPONSOR

Study Record Dates

• First Submitted: December 6, 2024
• First Posted: December 18, 2024
• Study Start: December 12, 2024
• Primary Completion (Estimated): October 1, 2026
• Study Completion (Estimated): December 1, 2026
• Last Updated: May 14, 2026

Record last verified: 2026-05

Locations

CN (1)