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Investigation of Anti-tumour Effect and Tolerability of the PARP Inhibitor 2X-121 in Patients With Metastatic Breast Cancer Selected by the 2X-121 DRP

Phase 2
Completed
Conditions
Metastatic Breast Cancer
Interventions
Registration Number
NCT03562832
Lead Sponsor
Allarity Therapeutics
Brief Summary

2X-121 is a small molecule targeted inhibitor of Poly ADP ribose polymerase (PARP), a key enzyme involved in DNA damage repair in cancer cells. The PARP inhibitor demonstrated clinical activity in a prior Phase 1 study in a number of solid tumors. 2X-121 has a novel dual-inhibitory action against both PARP 1/2 and Tankyrase 1/2. The molecule is also active in P-glycoprotein expressing cells, suggesting it may overcome some of the PARP inhibitor resistance.

The Phase 2 study is using 2x-121 DRP® biomarker in metastatic breast cancer patients to identify patients likely to respond to and benefit from treatment with 2X-121.

Detailed Description

Not available

Recruitment & Eligibility

Status
COMPLETED
Sex
All
Target Recruitment
20
Inclusion Criteria
  • Signed informed consent form.

  • Age 18 years or older.

  • Histologically or cytological documented mBC (independent of hormone receptor, HER2 status and BRCA1 or 2 status) relapsed in 2 or more different prior therapies.

  • Measurable disease by CT scan or MRI.

  • With a drug response prediction (DRP) for 2X-121 with an outcome measured as being in the upper 20% likelihood of response.

  • Prior chemotherapy or hormone therapy for metastatic breast cancer is allowed.

  • Performance status of ECOG <= 1

  • Recovered to Grade 1 or less from prior surgery or from acute toxicities of prior radiotherapy, or from treatment with cytotoxic, hormonal or biologic agents).

  • >= 2 weeks must have elapsed since any prior surgery or therapy with G-CSF and GM-CSF.

  • Patients with intracranial disease must be on stable or decreased level of steroid therapy (e.g. dexamethasone) for at least 7 days prior to baseline MRI. Non-enzymatic inducing ant-epileptic drugs are allowed.

  • Adequate conditions as evidenced by the following clinical laboratory values:

    • Absolute neutrophils count (ANC) >= 1.5 x 10E9/L
    • Haemoglobin is at least 4.6 mmol/L
    • Platelets >= 100 x 10E9 /L
    • Alanine aminotransferase (ALT) and aspartate aminotransferase (AST) <= 2.5 x ULN*
    • Serum bilirubin <= 1.5 ULN
    • Alkaline phosphatase <= 2.5 x ULN*
    • Creatinine <= 1.5 ULN
    • Blood urea within normal limits
    • Creatinine clearance within normal limits. *In case of known liver metastases with ALT and AST <= 5 x ULN and/or alkaline phosphatase <= 5 x ULN. Patients who do not conform to the transaminase and/or alkaline phosphatase inclusion criteria, but who by the PI are considered in good PS and otherwise eligible for inclusion, and where the transaminase and/or alkaline phosphatase levels are considered elevated due to other reasons than deteriorated lever capacity, may be considered for inclusion based on conferred agreement between PI and sponsor.
  • Life expectancy equal or longer than 3 months.

  • Sexually active females of child-producing potential must use adequate contraception (oral contraceptives, intrauterine device or barrier method of contraception) for the study duration and at least six months afterwards.

Exclusion Criteria
    • Concurrent chemotherapy, radiotherapy, hormonal therapy, or other investigational drug except non-disease related conditions (e.g. insulin for diabetes) during study period.
  • Other malignancy with exception of curative treated non-melanoma skin cancer or cervical carcinoma in situ within 5 years prior to entering the study.

  • Previous treatment with PARP inhibitors

  • Any active infection requiring parenteral or oral antibiotic treatment.

  • Has known HIV positivity.

  • Has known active hepatitis B or C.

  • Has clinical significant (i.e. active) cardiovascular disease:

    • Stroke within <= 6 months prior to day 1
    • Transient ischemic attach (TIA) within <= 6 months prior to day 1
    • Myocardial infarction within <= 6 months prior to day 1
    • Unstable angina
    • New York Hart Association (NYHA) Grade II or greater congestive heart failure (CHF)
    • Serious cardiac arrhythmia requiring medication
  • Mental status is not fit for clinical study or CNS disease including symptomatic epilepsy.

  • Other medications or conditions, including surgery, that in the Investigator's opinion would contraindicate study participation of safety reasons or interfere with the interpretation of study results

  • Inability to take oral medication, or malabsorption syndrome or any other uncontrolled gastrointestinal condition (e.g., nausea, diarrhea, or vomiting) that might impair the bioavailability of 2X-121.

  • Requiring immediate palliative treatment of any kind including surgery and/or radiotherapy.

  • Female patients who are pregnant or breast-feeding (pregnancy test with a positive result before study entry)

Study & Design

Study Type
INTERVENTIONAL
Study Design
SINGLE_GROUP
Arm && Interventions
GroupInterventionDescription
PARP inhibitor 2X-121PARP inhibitor 2X-121600 mg PARP inhibitor 2X-121 as single daily oral agent in mBC patients
Primary Outcome Measures
NameTimeMethod
Anti-tumour efficacy after treatment with 600 mg 2X-121 as single oral agent in a 21-days cycle in mBC patients selected by the 2X-121 DRPone year

Overall tumor response according to RECIST

Secondary Outcome Measures
NameTimeMethod
Progression free survival (PFS) after administration of 2X-121 in patients with mBCone year

Timespan

Duration of objective response after administration of 2X-121 in patients with mBCone year

Timespan

Overall survival (OS) after administration of 2X-121 in patients with mBCone year

Timespan

Number of participants with treatment-related adverse events as assessed by CTCAE v4.0one year

Adverse Events as assessed by CTCAE v4. to evaluate safety profile after administration of 2X-121 in patients with mBC

Performance status (ECOG)one year

To evaluate change in patient performance status by ECOG (Eastern Cooperative Oncology Group) Performance Status by a 6-step classification system

Trial Locations

Locations (2)

Vejle Sygehus

🇩🇰

Vejle, Denmark

Herlev and Gentofte Hospital, Herlev Ringvej 75, DK-2730 Herlev

🇩🇰

Herlev, Denmark

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