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A Phase 1/2 Trial of SRA737 in Subjects With Advanced Cancer

Phase 1
Completed
Conditions
Advanced Solid Tumors or Non-Hodgkin's Lymphoma (NHL)
Interventions
Registration Number
NCT02797964
Lead Sponsor
Sierra Oncology LLC - a GSK company
Brief Summary

The purpose of this clinical study is to establish the safety profile, determine the maximum tolerated dose (MTD) and recommend a Phase 2 dose and schedule of SRA737; and to evaluate the efficacy of SRA737 in prospectively-selected subjects with genetically-defined tumors that harbor genomic alterations linked to increased replication stress and that are hypothesized to be more sensitive to checkpoint kinase 1 (Chk1) inhibition via synthetic lethality. Specific cancer indications that frequently harbor these genetic mutations will be studied.

Detailed Description

SRA737 is a potent, highly selective, orally bioavailable small molecule inhibitor of Chk1, a key regulator of cell cycle progression and the DNA Damage Response (DDR) replication stress response. In cancer cells, intrinsic replication stress (RS) is induced by factors such as oncogenes (e.g., CCNE1 or MYC), genetic mutations in DNA repair machinery (e.g. BRCA1 or FANCA), genetic mutations leading to a dysregulated cell cycle (e.g., TP53 or RAD50) or other genomic alterations. This replication stress results in persistent DNA damage and genomic instability, leading to an increased dependency on Chk1 for survival. Targeted inhibition of Chk1 by SRA737 may therefore be synthetically lethal to cancer cells with elevated intrinsic RS.

This study has been designed to: establish the safety profile; determine the pharmacokinetic profile; identify the optimal dose, schedule, and MTD; obtain preliminary evidence of activity; and evaluate SRA737's efficacy in prospectively-selected subjects with tumors that harbor genomic alterations linked to increased replication stress and that are hypothesized to be more sensitive to Chk1 inhibition via synthetic lethality.

This clinical study consists of two phases, a Dose Escalation Phase 1 portion and a Cohort Expansion Phase 2 portion.

In the Dose Escalation Phase 1 portion, cohorts consisting initially of a single subject will receive escalating doses of SRA737, administered orally on a continuous daily dosing schedule in 28-day cycles. Once an SRA737-related Grade 2 toxicity is observed in a dose escalation cohort during Cycle 1, that cohort will be expanded to 3 to 6 subjects, and subsequent dose level cohorts will follow a rolling 6 design until the MTD has been identified.

In the Cohort Expansion Phase 2 portion, subjects with genetically-defined tumors that harbor genomic alterations linked to increased replication stress and that are hypothesized to be more sensitive to Chk1 inhibition will be prospectively enrolled into six indication-specific cohorts to explore the preliminary efficacy of SRA737. Subjects must have advanced or metastatic disease of one of the following types:

* castration-resistant prostate cancer (mCRPC);

* high grade serous ovarian cancer (HGSOC) without CCNE1 gene amplification;

* HGSOC with CCNE1 gene amplification (or alternative genetic alteration with similar functional effect);

* non-small cell lung cancer (NSCLC);

* head and neck squamous cell carcinoma (HNSCC) or squamous cell carcinoma of the anus (SCCA); and

* colorectal cancer (mCRC).

To qualify for enrolment in the Cohort Expansion Phase 2 portion, the subject's tumor must have a confirmed combination of mutations which are expected to confer sensitivity to Chk1 inhibition, determined by the Sponsor's review of genetic abnormalities detected in the following categories:

* Oncogenic drivers such as CCNE1 or MYC, etc.

* Genes involved in the DNA repair process including BRCA1, BRCA2, FANC genes, mismatch repair (MMR) genetic alterations and/or high microsatellite instability.

* Key tumor suppressor genes regulating G1 cell cycle progression/arrest such as TP53, RAD50, etc. For patients with HNSCC or SCCA, positive human papilloma virus (HPV) status is also considered for eligibility.

* Genetic indicators of replicative stress such as gain of function/amplification of CHEK1, ATR or other related genes.

Tumor genetics will be prospectively determined using Next-Generation Sequencing.

Recruitment & Eligibility

Status
COMPLETED
Sex
All
Target Recruitment
107
Inclusion Criteria
  1. For Dose Escalation Only: any locally advanced or metastatic, histologically or cytologically proven solid tumor or NHL, relapsed after or progressing despite conventional treatment
  2. Life expectancy of at least 12 weeks
  3. World Health Organization (WHO) performance status of 0-1
  4. Must meet select hematological and biochemical laboratory indices
  5. Archival tumor tissue or accessible tumor and willingness to consent to a biopsy

Expansion Only:

  1. Any locally advanced or metastatic malignancy of the following types for which no other conventional therapy is considered appropriate:

    • Metastatic Colorectal Cancer (CRC)
    • Platinum-resistant or intolerant High Grade Serious Ovarian Cancer (HGSOC)
    • Advanced Non-Small Cell Lung Cancer (NSCLC)
    • Metastatic Castration-Resistant Prostate Cancer (mCRPC)
    • Head and Neck Squamous Cell Carcinoma (HNSCC) or squamous cell carcinoma of the anus (SCCA).
    • Eligibility may be further restricted by the select number of prior regimens specific to each indication
  2. Measurable disease per RECIST v1.1, or for mCRPC, evaluable disease per any of the following:

    • Measurable disease per RECIST v1.1
    • Increasing PSA
    • Circulating tumor cell (CTC) count of 5 or more cells per 7.5 ml of blood
  3. Tumor tissue or ctDNA evidence that subject's tumor harbors a combination of mutations which are expected to confer sensitivity to Chk1 inhibition. Eligibility will be determined by the Sponsor's review of genetic abnormalities detected in genes in the following categories:

    • Oncogenic drivers such as MYC, CCNE1, etc.
    • Key tumor suppressor genes regulating G1 cell cycle progression/arrest such as RAD50, TP53, etc. For patients with NHSCC or SCCA, positive HPV status is also considered for eligibility.
    • The DDR pathway including BRCA1, BRCA2 and FANC. For patients with CRC, MMR genetic alterations and/or high microsatellite instability are also considered for eligibility.
    • Genetic indicators of replicative stress such as gain of function/amplification of Chk1 or ATR or other related gene.

Key

Exclusion Criteria
  1. Received the following prior or current anticancer therapy:

    • Radiotherapy within the last 6 weeks
    • Endocrine therapy during the previous 4 weeks
    • Chemotherapy during the previous 4 weeks
    • Immunotherapy during the previous 6 weeks
    • Nitrosoureas or Mitomycin C during the previous 6 weeks
    • Other Investigational Medicinal Product during the 4 weeks before treatment
    • Any prior treatment with a Chk1 inhibitor or prior treatment with an ATR inhibitor within 6 months prior to receiving SRA737
  2. Other malignancy within the past 2 years, except for adequately treated tumors

  3. Ongoing toxic manifestations of previous treatments greater than NCI-CTCAE Grade 1

  4. For Dose Escalation: new or progressing brain metastases. For Cohort Expansion: present or prior brain metastases

  5. High medical risk because of nonmalignant systemic disease

  6. Serologically positive for hepatitis B, hepatitis C or HIV

  7. Serious cardiac condition, left ventricular ejection fraction < 45% at baseline, history of cardiac ischemia within the past 6 months, or prior history of cardiac arrhythmia requiring treatment

  8. Prior bone marrow transplant or extensive radiotherapy to greater than 25% of bone marrow within 8 weeks

  9. Peanut allergy

  10. QTcF> 450 msec in adult males and > 470 msec in adult females

  11. Impairment of gastrointestinal (GI) function or GI disease that may significantly alter the absorption of SRA737

  12. Inability to swallow capsules without chewing or crushing

  13. Is a participant or plans to participate in another interventional clinical trial

  14. Any other condition which in the Investigator's opinion would not make the subject a good candidate

Study & Design

Study Type
INTERVENTIONAL
Study Design
SEQUENTIAL
Arm && Interventions
GroupInterventionDescription
Open labelSRA737-
Primary Outcome Measures
NameTimeMethod
Number of Subjects With Adverse Events as Assessed by CTCAE 4.03Up to 30 days after last dose of SRA737

Treatment-emergent adverse events (TEAEs) were reported until the safety Follow up (SFU) visit, 30 days after the last dose of SRA737 or prior to the initiation of a new anticancer treatment, whichever came first.

Maximum Tolerated Dose of SRA737Cycle 1 (28 days) in the Dose Escalation Phase

The highest dose at which ≤ 33% of subjects have a dose limiting toxicity (DLT) in a cohort of up to 6 subjects.

Recommended Phase 2 Dose of SRA737Up to 30 days after last dose of SRA737

The RP2D and schedule were defined by the Cohort Review Committee at the end of the study and took all clinically relevant toxicity, PK and PDn data into account. The RP2D was to be a dose equal to or less than the MTD for the selected schedule.

Disease Control Rate (DCR) of SRA737Radiographic tumor assessments were performed every 2 cycles of therapy.

The disease control rate (DCR) was defined as the number of subjects achieving complete response (CR) + partial response (PR) + stable disease (SD) per RECIST 1.1 criteria. Since no subjects achieved CR or PR in this study, the DCR represents the proportion of subjects in each group who achieved SD.

Time to Progression (TTP)Radiographic tumor assessments were performed every 2 cycles of therapy. Follow-up assessments were made every 16 weeks for subjects who had not progressed and had not initiated new anticancer therapy.

Time to progression (TTP) was defined as the time from Cycle 1 Day 1 to the earliest date of radiographic disease progression per RECIST 1.1, or if the subject did not experience disease progression, to the last imaging assessment. TTP was analyzed using the K-M method.

Progression Free Survival (PFS)Radiographic tumor assessments were performed every 2 cycles of therapy. Follow-up assessments were made every 16 weeks for subjects who had not progressed and had not initiated new anticancer therapy.

Progression free survival (PFS) was defined as time from Cycle 1 Day 1 to the earliest date of radiographic disease progression per RECIST 1.1 or death, whichever happened first. Censoring rules are defined in the SAP. PFS was analyzed using the K-M method.

Overall Survival (OS)Follow-up assessments were made every 16 weeks for subjects who had not progressed and had not initiated new anticancer therapy.

Overall survival (OS) was defined as time from Cycle 1 Day 1 to the date of death (or date last known to be alive). OS was analyzed using the K-M method.

Secondary Outcome Measures
NameTimeMethod

Trial Locations

Locations (15)

Royal Marsden Hospital

🇬🇧

Sutton, London, United Kingdom

The Beatson West of Scotland Cancer Centre

🇬🇧

Glasgow, United Kingdom

Velindre Cancer Centre - Cardiff

🇬🇧

Cardiff, Whitchurch, United Kingdom

Oxford University Hospitals

🇬🇧

Headington, Oxford, United Kingdom

Western General Hospital

🇬🇧

Edinburgh, United Kingdom

The Leeds Teaching Hospitals of St James University Hospital

🇬🇧

Leeds, United Kingdom

University College London Hospitals

🇬🇧

London, United Kingdom

Sarah Cannon Research Institute

🇬🇧

London, United Kingdom

Guy's and St. Thomas

🇬🇧

London, United Kingdom

University Hospitals of Leicester

🇬🇧

Leicester, United Kingdom

The Christie

🇬🇧

Manchester, United Kingdom

Freeman Hospital

🇬🇧

Newcastle upon Tyne, United Kingdom

Sheffield Teaching Hospitals

🇬🇧

Sheffield, United Kingdom

The Clatterbridge Cancer Centre

🇬🇧

Bebington, Wirral, United Kingdom

Belfast City Hospital

🇬🇧

Belfast, Northern Ireland, United Kingdom

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