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Combination of 177Lu-TLX250 and Peposertib in Patients With Carbonic Anhydrase IX -Expressing Solid Tumors

Phase 1
Recruiting
Conditions
Advanced Solid Tumor
Advanced Renal Cell Carcinoma
Solid Tumor, Adult
Interventions
Diagnostic Test: 89Zr-TLX250
Combination Product: 177Lu-TLX250 and Peposertib
Registration Number
NCT05868174
Lead Sponsor
Telix Pharmaceuticals (Innovations) Pty Limited
Brief Summary

This is an open label, single-arm, multicentre dose escalation (Part 1) and dose expansion (Part 2) study to evaluate different combinations of 3 radioactive dose levels of 177Lu-TLX250 administered intravenously with 3 different doses of peposertib in patients with CAIX-expressing solid tumors.

Detailed Description

Part 1 (dose escalation) will evaluate the combination of 3 different activities of 177Lu-TLX250 and 3 different dose levels of peposertib.

Patients with CAIX positive solid tumors will be enrolled in a given dose/activity level in Cohorts of approximately 2-6 patients.

Treatment cycles will have a fixed length of 84 days. Patients will be treated during 3 cycles, or until clinically significant progression or unacceptable toxicity.

Part 2 (dose expansion) patients will be enrolled in 2 Cohorts:

* Cohort A: 40 patients with metastatic or non-resectable ccRCC

* Cohort B: 20 patients with CAIX-positive solid tumors (excluding RCC).

Patients will be treated at the Recommended phase 2 dose of 177Lu-TLX250 in combination with peposertib at the dosing schedule of the selected Recommended phase 2 dose.

Recruitment & Eligibility

Status
RECRUITING
Sex
All
Target Recruitment
36
Inclusion Criteria
  • Histologically confirmed advanced or metastatic solid tumor that has progressed on or during/after recognized standard of care therapies and are not eligible for resection, or patients that are not eligible or not consenting to recognized standard of care therapies.
  • At least one measurable lesion on CT/MRI according to RECIST 1.1 with corresponding 89Zr-TLX250 uptake (i.e., CAIX positive).
  • CAIX positivity in at least 75% of the total lesion volume (defined as 89Zr- TLX250 uptake with intensity significantly greater than normal liver [i.e., standardized uptake value [SUV]max at least 1.5 times SUV of normal liver]).
  • ECOG status 0 or 1.
  • Have adequate organ function during screening
  • Must have a life expectancy of at least 6 months.
Exclusion Criteria
  • Prior 177Lu-TLX250 or other radioligand therapy; or any prior CAIX targeting therapy.
  • Known hypersensitivity to compounds of similar chemical or biologic composition to peposertib, girentuximab radiolabelled by zirconium or lutetium, any excipient in the study medication or any other intravenously administered human proteins/peptides/antibodies.
  • Administration of any radionuclide within 10 half-lives of the radionuclide prior to signature of the ICF.
  • Patients who have had chemotherapy, definitive radiation, biological cancer therapy, or investigational agent/device within 28 days of first planned dose of study therapy.
  • Patients who had > 2 prior lines of cytotoxic chemotherapy or had Grade 4 neutropenia or Grade 3/Grade 4 thrombocytopenia (both of a duration of at least 48 hours) during the last line of therapy. Note: This criterion may be removed in total or in part by the SRC upon review of the safety data from the initial dose level(s).
  • Patients who cannot discontinue concomitant medications or herbal supplements that are strong inhibitors or strong inducers of cytochrome P450 (CYP) isoenzymes CYP3A4/5, CYP2C9, and CYP2C19. Concomitant use of CYP3A4/5 substrates with a narrow therapeutic index are also excluded.
  • Patients who cannot discontinue concomitant H2-blockers or proton-pump inhibitors (PPIs). Patients may confer with the investigator to determine if such medications can be discontinued. These must be discontinued ≥ 5 days prior to study treatment. Patients do not need to discontinue calcium carbonate.
  • Patients who are receiving therapeutic doses of anticoagulation, including but not limited to low-molecular weight heparin in therapeutic dosing or platelet aggregation inhibitors. Note: This criterion may be removed by the SRC upon review of the safety data from the initial dose level(s).
  • Patients with ≥ 5 bone metastases and/or bulky (> 3cm in diameter) pelvic or femoral tumors, and/or metastases/tumor in the vertebral spine involving > 3 vertebrae.
  • Any severe concomitant condition which makes it undesirable for the patient to participate in the study or which could jeopardize compliance with the protocol, in the opinion of the investigator.
  • Presence of active and uncontrolled infections or other severe concurrent disease, which, in the opinion of the investigator, would place the patient at undue risk or interfere with the study.
  • Requirement of concurrent use of other anti-cancer treatments or agents other than study medications. Supportive care therapies are permitted.

Study & Design

Study Type
INTERVENTIONAL
Study Design
SEQUENTIAL
Arm && Interventions
GroupInterventionDescription
89Zr-TLX250, 177Lu-TLX250 and Peposertib89Zr-TLX250Diagnostic test: A single IV administration of 37 Megabecquerel (+/- 10%) 89Zr-DFO-girentuximab, containing a mass dose of 10 mg of girentuximab, followed by a diagnostic scan Treatment test: A single IV administration that could be 1887 - 2516 or 3145 Megabecquerel (+/- 10%) 177Lu-DOTA-girentuximab,containing a mass dose of 10 mg of girentuximab, on Day 1 of each 84-day cycle and p.o. administration of that could be 100-150 or 200 mg Peposertib BID on days 4-21 of each 84-day cycle.
89Zr-TLX250, 177Lu-TLX250 and Peposertib177Lu-TLX250 and PeposertibDiagnostic test: A single IV administration of 37 Megabecquerel (+/- 10%) 89Zr-DFO-girentuximab, containing a mass dose of 10 mg of girentuximab, followed by a diagnostic scan Treatment test: A single IV administration that could be 1887 - 2516 or 3145 Megabecquerel (+/- 10%) 177Lu-DOTA-girentuximab,containing a mass dose of 10 mg of girentuximab, on Day 1 of each 84-day cycle and p.o. administration of that could be 100-150 or 200 mg Peposertib BID on days 4-21 of each 84-day cycle.
Primary Outcome Measures
NameTimeMethod
Safety parameter Dose Limited Toxicity (DLT)42 days

Dose level toxicity evaluation using Partial Ordering Bayesian Logistic Regression Model Method (PO-BLRM)

Disease impact causing changes in Eastern Cooperative Oncology Group (ECOG) Performance scale.Screening/Baseline, Day1, Day 29, D57 and End of Treatment

Quality of life ( in terms of their ability to care for themself, daily activity, and physical ability (walking, working) is to be evaluated using the ECOG Performance Scale.

Safety parameter Adverse Events and Treatment-Related Adverse Events42 days

Assessment of AEs graded by the Common Terminology Criteria for Adverse Events (CTCAE) Criteria, Version 5.0

Safety parameter Laboratory Examinations42 days

Frequency of occurrence and severity of abnormal findings in safety investigations regarding Laboratory examinations

Safety parameter ECG42 days

Frequency of occurrence and severity of abnormal findings in the 12-lead ECG (ECG QT interval)

Safety parameter Vital signs42 days

Frequency of occurrence and severity of abnormal findings in safety investigations regarding the vital signs

Secondary Outcome Measures
NameTimeMethod
Immunogenicity by formation of ADA(HACA) in blood84 days

This outcome will be measured by analyzing the incidence of ADA(HACA) formation in blood on day 1, day 22, Day 43, Day 57 of each cycle (each cycle is 84 days) and at the end of treatment visit.

Tumor objective response rate (ORR)Every 3 months ± 2 weeks for 12 months after the last 177Lu-TLX250 administration

Tumor response in terms of objective response rate (ORR) (solid tumor tissue response and overall radiological response \[tumor response by RECIST 1.1 and overall radiological response by RECIST 1.1\])

Overall Survival (OS)Every 3 months ± 2 weeks for 24 months after the last 177Lu-TLX250 administration

Overall Survival (OS), determined from enrollment , until death from any cause

Progression-free survival (PFS)Every 3 months ± 2 weeks for 12 months after the last 177Lu-TLX250 administration

Progression free survival (PFS) defined as the time from enrollment to disease progression confirmed by radiology, clinical progression or death (whichever comes first)

Trial Locations

Locations (5)

Macquarie University

🇦🇺

North Ryde, New South Wales, Australia

Ashford (Icon) Cancer Centre

🇦🇺

Adelaide, Australia

Princess Alexandra Hospital

🇦🇺

Brisbane, Australia

GenesisCare Murdoch

🇦🇺

Perth, Australia

Austin Health

🇦🇺

Melbourne, Australia

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