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Study of AVZO-021 in Patients With Advanced Solid Tumors

Phase 1
Recruiting
Conditions
Advanced Solid Tumor
HR+/HER2- Breast Cancer
HR+, HER2-, Advanced Breast Cancer
CCNE1 Amplification
Epithelial Ovarian Cancer
Primary Peritoneal Cancer
Fallopian Tube Cancer
Endometrial Cancer
TNBC - Triple-Negative Breast Cancer
Interventions
Registration Number
NCT05867251
Lead Sponsor
Avenzo Therapeutics, Inc.
Brief Summary

This study, the first clinical trial of AVZO-021, aims to determine the safety, tolerability, pharmacokinetics, pharmacodynamics, maximum tolerated dose, and anti-tumor effects of AVZO-021 in patients with advanced solid tumors. AVZO-021 is an oral medication that inhibits cyclin-dependent kinase 2 (CDK 2).

Detailed Description

AVZO-021 is a compound being developed for the treatment of patients with advanced solid tumors, specifically, HR+/HER2- breast cancer and cyclin E1 (CCNE1) altered malignancies. AVZO-021 is a selective and potent cyclin-dependent kinase 2 (CDK2) inhibitor, which plays an important role in cell cycle regulation. This is a Phase 1/2 first-in-human, open-label, nonrandomized, multicenter study of AVZO-021. Phase 1 is a dose-escalation phase aimed at assessing the safety and tolerability of AVZO-021 and determining the recommended phase 2 dose (RP2D) as monotherapy and combination therapy. Phase 2 is a dose-expansion phase that will be conducted to assess the antitumor activity of AVZO-021 as monotherapy and combination therapy.

Recruitment & Eligibility

Status
RECRUITING
Sex
All
Target Recruitment
430
Inclusion Criteria
  1. Male or female aged ≥18 years old at screening with Eastern Cooperative Oncology Group (ECOG) 0-1.

  2. Disease-related inclusion criteria by study phase and part:

    i) Phase 1a Monotherapy Dose Escalation: Patients with locally advanced or metastatic HR+/HER2- breast cancer, CCNE1-amplified tumors that are either epithelial ovarian cancer, primary peritoneal cancer, fallopian tube cancer, endometrial cancer or TNBC, with no other oncogenic driver mutations that are treatable and standard therapies are no longer effective, appropriate, or safe in the opinion of the investigator and medical monitor. Patients with any additional tumor type with CCNE1 amplification can be enrolled only if clinical data is supportive and approved by medical monitor (Cohort 1A).

    ii) Phase 1b Combination Dose Escalation: histologically or cytologically confirmed diagnosis of locally advanced or metastatic HR+ HER2- (HER2-low may be allowed if failed standard of care therapy) breast cancer, who have been previously treated with inhibitor of CDK4/6 and endocrine therapy(Cohorts 1B1, 1B2, 1B3, 1B4, and 1B5); or histologically or cytologically confirmed diagnosis of CCNE1- amplified, locally advanced or metastatic, platinum-refractory or platinum-resistant EOC, primary peritoneal, or fallopian tube cancer (Cohort 1C).

    iii) Phase 2a Monotherapy dose expansion: Histologically or cytologically confirmed diagnosis of locally advanced or metastatic CCNE1 amplified epithelial ovarian cancer, primary peritoneal cancer, fallopian tube cancer, endometrial cancer or TNBC, with no other oncogenic driver mutations that are treatable and standard therapies are no longer effective, appropriate, or safe in the opinion of the investigator and medical monitor (Cohort 2A).

    iv) Phase 2b Combination dose expansion: Histologically or cytologically confirmed diagnosis of locally advanced or metastatic HR+/HER2- (HER2-low may be allowed if failed standard of care therapy) breast cancer who have been previously treated with no more than 1 prior CDK4/6 inhibitor and endocrine therapy (Cohorts 2B1, 2B2, 2B3, 2B4, and 2B5); or Histologically or cytologically confirmed diagnosis of locally advanced or metastatic, CCNE1-amplified, platinum-refractory or platinum-resistant EOC, primary peritoneal cancer, or fallopian tube cancer (Cohort 2C).

  3. No more than 2 prior cytotoxic chemotherapy regimens for locally advanced/metastatic disease (excepting patients treated with an antibody-drug conjugate, with ovarian cancer if there disease is platinum resistant or refractory, having progressed beyond all SOC care; and patients who have received prior chemotherapy in the adjuvant or neoadjuvant setting >12 months prior to starting AVZO-021 treatment).

  4. Measurable disease as determined by RECIST version 1.1.

  5. Adequate bone marrow and organ function.

  6. Ability to swallow capsules or tablets.

Key

Exclusion Criteria
  1. Received an investigational agent or anticancer therapy within 2 weeks, or 5 half-lives of the drug, whichever is shorter, prior to planned start of AVZO-021.
  2. Received any CDK2 inhibitor, protein kinase membrane associated tyrosine/threonine 1 (PKMYT1) inhibitor, or WEE1 inhibitor anticancer therapy. For cohort B5, prior therapy with topoisomerase inhibitors is not permitted.
  3. Undergone major surgery within 4 weeks prior to planned start of AVZO-021.
  4. Received radiotherapy for palliation within 7 days of the first dose of study treatment, unless specified otherwise in the protocol.
  5. Active CNS metastases or confirmed leptomeningeal disease are not eligible.
  6. Unresolved toxicities from prior therapy greater than Common Terminology Criteria for Adverse Events (CTCAE) version 5.0 Grade >1 at the time of starting study treatment.
  7. Clinically unstable cardiac function as described in the protocol.
  8. Any active or chronic infection/disease that compromises the immune system.
  9. Current treatment with strong or moderate cytochrome P450 (CYP)3A4 inhibitors or inducers.
  10. Active second malignancy unless in remission with life expectancy > 2 years and with documented sponsor approval.
  11. Pregnancy, lactation, or plans to breastfeed during the study or within 6 months of the last dose of study intervention.

Study & Design

Study Type
INTERVENTIONAL
Study Design
SEQUENTIAL
Arm && Interventions
GroupInterventionDescription
Phase 1, combination (Parts 1B and 1C)AVZO-021Escalating doses of once daily, oral AVZO-021 in 28-day cycles starting at least 1 DL below the monotherapy MTD/RP2D dose in combination with: 1B1) fulvestrant 1B2) palbociclib plus either fulvestrant or letrozole 1B3) ribociclib plus either fulvestrant or letrozole 1B4) abemaciclib plus either fulvestrant or letrozole 1B5) sacituzumab govitecan-hziy 1C) carboplatin
Phase 2, monotherapy (Part 2A)AVZO-021Oral doses of AVZO-021 in 28-day cycles at the RP2D determined in Part 1A.
Phase 2, combination (Parts 2B and 2C)AVZO-021Oral doses of AVZO-021 in 28-day cycles at the RP2D determined in Parts 1B/1C, in combination with: 2B1) fulvestrant 2B2) palbociclib plus either fulvestrant or letrozole 2B3) ribociclib plus either fulvestrant or letrozole 2B4) abemaciclib plus either fulvestrant or letrozole 2B5) sacituzumab govitecan-hziy 2C) carboplatin
Phase 1, monotherapy (Part 1A)AVZO-021Escalating doses of once daily, oral AVZO-021 in 28-day cycles.
Phase 1, combination (Parts 1B and 1C)PalbociclibEscalating doses of once daily, oral AVZO-021 in 28-day cycles starting at least 1 DL below the monotherapy MTD/RP2D dose in combination with: 1B1) fulvestrant 1B2) palbociclib plus either fulvestrant or letrozole 1B3) ribociclib plus either fulvestrant or letrozole 1B4) abemaciclib plus either fulvestrant or letrozole 1B5) sacituzumab govitecan-hziy 1C) carboplatin
Phase 1, combination (Parts 1B and 1C)FulvestrantEscalating doses of once daily, oral AVZO-021 in 28-day cycles starting at least 1 DL below the monotherapy MTD/RP2D dose in combination with: 1B1) fulvestrant 1B2) palbociclib plus either fulvestrant or letrozole 1B3) ribociclib plus either fulvestrant or letrozole 1B4) abemaciclib plus either fulvestrant or letrozole 1B5) sacituzumab govitecan-hziy 1C) carboplatin
Phase 1, combination (Parts 1B and 1C)LetrozoleEscalating doses of once daily, oral AVZO-021 in 28-day cycles starting at least 1 DL below the monotherapy MTD/RP2D dose in combination with: 1B1) fulvestrant 1B2) palbociclib plus either fulvestrant or letrozole 1B3) ribociclib plus either fulvestrant or letrozole 1B4) abemaciclib plus either fulvestrant or letrozole 1B5) sacituzumab govitecan-hziy 1C) carboplatin
Phase 1, combination (Parts 1B and 1C)RibociclibEscalating doses of once daily, oral AVZO-021 in 28-day cycles starting at least 1 DL below the monotherapy MTD/RP2D dose in combination with: 1B1) fulvestrant 1B2) palbociclib plus either fulvestrant or letrozole 1B3) ribociclib plus either fulvestrant or letrozole 1B4) abemaciclib plus either fulvestrant or letrozole 1B5) sacituzumab govitecan-hziy 1C) carboplatin
Phase 1, combination (Parts 1B and 1C)AbemaciclibEscalating doses of once daily, oral AVZO-021 in 28-day cycles starting at least 1 DL below the monotherapy MTD/RP2D dose in combination with: 1B1) fulvestrant 1B2) palbociclib plus either fulvestrant or letrozole 1B3) ribociclib plus either fulvestrant or letrozole 1B4) abemaciclib plus either fulvestrant or letrozole 1B5) sacituzumab govitecan-hziy 1C) carboplatin
Phase 1, combination (Parts 1B and 1C)CarboplatinEscalating doses of once daily, oral AVZO-021 in 28-day cycles starting at least 1 DL below the monotherapy MTD/RP2D dose in combination with: 1B1) fulvestrant 1B2) palbociclib plus either fulvestrant or letrozole 1B3) ribociclib plus either fulvestrant or letrozole 1B4) abemaciclib plus either fulvestrant or letrozole 1B5) sacituzumab govitecan-hziy 1C) carboplatin
Phase 1, combination (Parts 1B and 1C)Sacituzumab Govitecan-hziyEscalating doses of once daily, oral AVZO-021 in 28-day cycles starting at least 1 DL below the monotherapy MTD/RP2D dose in combination with: 1B1) fulvestrant 1B2) palbociclib plus either fulvestrant or letrozole 1B3) ribociclib plus either fulvestrant or letrozole 1B4) abemaciclib plus either fulvestrant or letrozole 1B5) sacituzumab govitecan-hziy 1C) carboplatin
Phase 2, combination (Parts 2B and 2C)PalbociclibOral doses of AVZO-021 in 28-day cycles at the RP2D determined in Parts 1B/1C, in combination with: 2B1) fulvestrant 2B2) palbociclib plus either fulvestrant or letrozole 2B3) ribociclib plus either fulvestrant or letrozole 2B4) abemaciclib plus either fulvestrant or letrozole 2B5) sacituzumab govitecan-hziy 2C) carboplatin
Phase 2, combination (Parts 2B and 2C)FulvestrantOral doses of AVZO-021 in 28-day cycles at the RP2D determined in Parts 1B/1C, in combination with: 2B1) fulvestrant 2B2) palbociclib plus either fulvestrant or letrozole 2B3) ribociclib plus either fulvestrant or letrozole 2B4) abemaciclib plus either fulvestrant or letrozole 2B5) sacituzumab govitecan-hziy 2C) carboplatin
Phase 2, combination (Parts 2B and 2C)LetrozoleOral doses of AVZO-021 in 28-day cycles at the RP2D determined in Parts 1B/1C, in combination with: 2B1) fulvestrant 2B2) palbociclib plus either fulvestrant or letrozole 2B3) ribociclib plus either fulvestrant or letrozole 2B4) abemaciclib plus either fulvestrant or letrozole 2B5) sacituzumab govitecan-hziy 2C) carboplatin
Phase 2, combination (Parts 2B and 2C)RibociclibOral doses of AVZO-021 in 28-day cycles at the RP2D determined in Parts 1B/1C, in combination with: 2B1) fulvestrant 2B2) palbociclib plus either fulvestrant or letrozole 2B3) ribociclib plus either fulvestrant or letrozole 2B4) abemaciclib plus either fulvestrant or letrozole 2B5) sacituzumab govitecan-hziy 2C) carboplatin
Phase 2, combination (Parts 2B and 2C)AbemaciclibOral doses of AVZO-021 in 28-day cycles at the RP2D determined in Parts 1B/1C, in combination with: 2B1) fulvestrant 2B2) palbociclib plus either fulvestrant or letrozole 2B3) ribociclib plus either fulvestrant or letrozole 2B4) abemaciclib plus either fulvestrant or letrozole 2B5) sacituzumab govitecan-hziy 2C) carboplatin
Phase 2, combination (Parts 2B and 2C)CarboplatinOral doses of AVZO-021 in 28-day cycles at the RP2D determined in Parts 1B/1C, in combination with: 2B1) fulvestrant 2B2) palbociclib plus either fulvestrant or letrozole 2B3) ribociclib plus either fulvestrant or letrozole 2B4) abemaciclib plus either fulvestrant or letrozole 2B5) sacituzumab govitecan-hziy 2C) carboplatin
Phase 2, combination (Parts 2B and 2C)Sacituzumab Govitecan-hziyOral doses of AVZO-021 in 28-day cycles at the RP2D determined in Parts 1B/1C, in combination with: 2B1) fulvestrant 2B2) palbociclib plus either fulvestrant or letrozole 2B3) ribociclib plus either fulvestrant or letrozole 2B4) abemaciclib plus either fulvestrant or letrozole 2B5) sacituzumab govitecan-hziy 2C) carboplatin
Primary Outcome Measures
NameTimeMethod
Occurrence of Dose Limiting Toxicities (DLTs) during the first cycle (Phase 1)28 Days

Number of participants with DLTs assessed for severity using CTCAE v5.0 criteria will be summarized by dose level.

Number of Participants with Treatment Emergent Adverse Events (TEAEs) and lab abnormalities (Phase 1)Approximately 22 months

To evaluate the type, incidence, severity, timing, seriousness, and relationship to study treatment of adverse events and any laboratory abnormalities summarized by dose level.

Determination of Recommended Phase 2 Dose (RP2D) (Phase 1)Approximately 16 months

RP2D for AVZO-021 is less than or the same as the maximum tolerated dose (MTD) as defined by the occurrence of DLTs and TEAEs calculated using isotonic regression.

Objective Response Rate (ORR) (Phase 2)Approximately 52 months

Defined as the proportion of patients with a confirmed Complete Response (CR) or Partial Response (PR), as determined by the investigator by radiographic disease assessment according to RECIST v1.1.

Progression Free Survival (PFS) (Phase 2)Approximately 52 months

Defined as the time from study drug treatment to death or disease progression, as determined by the investigator by radiographic disease assessment according to RECIST v1.1.

Overall Survival (OS) (Phase 2)Approximately 76 months

Defined as the time from study drug treatment initiation to death from any cause.

Duration of response (DOR) (Phase 2)Approximately 52 months

Defined as the time from the first confirmed response to radiologic/objective progression.

Secondary Outcome Measures
NameTimeMethod
PK Parameters: Maximum plasma concentration (Cmax) (monotherapy and combination)Cycle 1 days 1, 2, 8, 14, and 15 (each cycle is 28 days)
PK Parameters: Time to maximum plasma concentration (Tmax) (monotherapy and combination)Cycle 1 days 1, 2, 8, 14, and 15 (each cycle is 28 days)
PK Parameters: Area under the plasma concentration-time curve from time 0 to last measurable concentration (AUC 0-last) (monotherapy and combination)Cycle 1 days 1, 2, 8, 14, and 15 (each cycle is 28 days)
PK Parameters: Area under the plasma concentration-time curve from time 0 to last measurable concentration (AUC 0-tau) (monotherapy and combination)Cycle 1 days 1, 2, 8, 14, and 15 (each cycle is 28 days)
PK Parameters: Minimum observed plasma concentration at steady state (Cmin, ss) (monotherapy and combination)Cycle 1 days 1, 2, 8, 14, and 15 (each cycle is 28 days)
PK Parameters: Elimination half-life (t1/2) (monotherapy and combination)Cycle 1 days 1, 2, 8, 14, and 15 (each cycle is 28 days)
PK Parameters: Accumulation ration (Rac) (monotherapy and combination)Cycle 1 days 1, 2, 8, 14, and 15 (each cycle is 28 days)
Evaluate the effect of a high-fat meal on the PK of AVZO-021 (Phase 1)5 days
PK Parameters: Apparent clearance (CL/F) (monotherapy and combination)Cycle 1 days 1, 2, 8, 14, and 15 (each cycle is 28 days)
PK Parameters: Apparent volume of distribution during terminal phase (Vz/F) (monotherapy and combination)Cycle 1 days 1, 2, 8, 14, and 15 (each cycle is 28 days)

Trial Locations

Locations (9)

Texas Oncology - DFW

🇺🇸

Dallas, Texas, United States

Yale Cancer Center

🇺🇸

New Haven, Connecticut, United States

Florida Cancer Specialists

🇺🇸

Sarasota, Florida, United States

Sidney Kimmel Cancer Center (SKCC) at Jefferson Health

🇺🇸

Philadelphia, Pennsylvania, United States

NEXT Virginia

🇺🇸

Fairfax, Virginia, United States

Macquarie University Hospital

🇦🇺

Macquarie University, New South Wales, Australia

University Hospitals Cleveland Medical Center

🇺🇸

Cleveland, Ohio, United States

Oklahoma University

🇺🇸

Oklahoma City, Oklahoma, United States

Cancer Care Wollongong

🇦🇺

Wollongong, New South Wales, Australia

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