Overview

Hydroxychloroquine, Abemaciclib and Endocrine Therapy in Hormone Receptor Positive (HR+)/Her 2 Negative Breast Cancer

Status:
Recruiting
Trial end date:
2028-01-01
Target enrollment:
0
Participant gender:
All
Summary
The hypothesis is that abemaciclib synergizes with autophagy inhibitor hydroxychloroquine (HCQ/ Plaquenil), inducing apoptosis leading to tumor regression.
Phase:
Phase 1
Accepts Healthy Volunteers?
No
Details
Lead Sponsor:
Medical College of Wisconsin
Treatments:
Anastrozole
Fulvestrant
Hydroxychloroquine
Letrozole
Criteria
Eligibility Criteria for Part 1 (Enrollment Criteria for the Dose-Escalation Cohort)

Inclusion Criteria for Dose-escalation Phase

1. Patients with advanced or metastatic cancers who are refractory to standard therapy,
relapsed after standard therapy, or who have no standard therapy available that
improves progression-free or overall survival by at least three months.

2. Intact G1/S checkpoint in tumor tissue defined by positive-Rb staining and
negative-low-molecule weight isoforms of cyclin E (LMWE) with staining done on
formalin-fixed paraffin embedded slides from archival tissue or cell blocks.

3. Demonstrate measurable disease as defined by Response Evaluation Criteria in Solid
Tumors (RECIST)1.1 criterion.

4. Age ≥ 18 years.

5. Estimated life expectancy of three months.

6. Eastern Cooperative Oncology Group (ECOG) performance status ≤2.

7. Patients with asymptomatic central nervous system (CNS) metastases not requiring use
of corticosteroids will be allowed.

8. Patients who received chemotherapy must have recovered (Common Terminology Criteria
for Adverse Events [CTCAE] Grade ≤1) from the acute effects of chemotherapy except for
residual alopecia or Grade 2 peripheral neuropathy prior to randomization. A washout
period of at least 21 days is required between the last chemotherapy dose and the
first dose of the study drug/s (provided the patient did not receive radiotherapy).

9. Patients who received palliative radiotherapy must have completed and fully recovered
from the acute effects of radiotherapy. A washout period of at least 14 days is
required between the end of radiotherapy and the first dose of the study drug/s.

10. Patients must be >/= 3 weeks from major surgery. For biologic/targeted agents,
patients must be >/= 5 half-lives or >/= 3 weeks from the last dose (whichever comes
first).

11. The patient is able to swallow oral medications.

12. Documented ophthalmic exam within the last 12 months demonstrating no evidence of
retinopathy. Patients with retinal changes will be considered for enrollment with
written clearance from a board-certified ophthalmologist.

13. The patient must sign informed consent prior to registration.

14. The patient has adequate organ function for all of the following criteria, as defined
below.

Laboratory Value Guidance to Establish Adequate Organ Function

Hematologic:

- Absolute Neutrophil Count (ANC) ≥ 1.5 × 109/L

- Platelets ≥100 × 109/L

- Hemoglobin ≥8 g/dL (Patients may receive erythrocyte transfusions to achieve this
hemoglobin level at the discretion of the investigator. Initial treatment must
not begin earlier than the day after the erythrocyte transfusion.)

Hepatic:

- Total bilirubin ≤1.5 × upper limit of normal (ULN)

- Patients with Gilbert's syndrome with a total bilirubin ≤2.0 times ULN and direct
bilirubin within normal limits are permitted.

- Alanine Aminotransferase (ALT) and aspartate aminotransferase (AST) ≤3 × ULN

Renal:

-Creatinine Clearance ≥30 mL/minute

15. Female subjects must meet one of the following:

- Postmenopausal for at least one year before enrollment, OR

- Surgically sterile (i.e., undergone a hysterectomy or bilateral oophorectomy), OR

- If subject is of childbearing potential (defined as not satisfying either of the
above two criteria), agrees to practice two acceptable methods of contraception
(combination methods require use of two of the following: diaphragm with
spermicide, cervical cap with spermicide, contraceptive sponge, male or female
condom, hormonal contraceptive) from the time of signing of the informed consent
form through 21 days after the last dose of study agent, OR

o Agrees to practice true abstinence when this is in line with the preferred and
usual lifestyle of the subject. (Periodic abstinence [e.g., calendar, ovulation,
symptothermal, postovulation methods] and withdrawal are not acceptable
contraception methods.)

16. Male subjects, even if surgically sterilized (i.e., status postvasectomy), must agree
to one of the following:

- Practice effective barrier contraception during the entire study period and
through 60 calendar days after the last dose of study agent, OR o Agree to
practice true abstinence when this is in line with the preferred and usual
lifestyle of the subject. (Periodic abstinence [e.g., calendar, ovulation,
symptothermal, post ovulation methods] and withdrawal are not acceptable methods
of contraception.)

Exclusion Criteria for Dose-escalation Phase

1. Serious concomitant systemic disorder that would compromise the safety of the patient
or compromise the patient's ability to complete the study, as determined by the
treating physician or the principal investigator (for example, interstitial lung
disease, severe dyspnea at rest, history of major surgical resection involving the
stomach or small bowel, or preexisting Crohn's disease or ulcerative colitis or a
preexisting chronic condition resulting in baseline grade 2 or higher diarrhea).

2. Second primary malignancy except most in situ carcinomas (e.g., adequately treated
non-melanomatous carcinoma of the skin) or other malignancy treated at least five
years previously with no evidence of recurrence.

3. Uncontrolled or symptomatic CNS metastases.

4. Known history of glucose-6-phosphate dehydrogenase (G6PD) deficiency.

5. Taking other commercially available medications, which may theoretically either
stimulate or inhibit autophagy; these include calcitriol and chloroquine.

6. Taking medications which may lead to interactions with HCQ, including penicillamine,
telbivudine, botulinum toxin, digoxin and propafenone.

7. Must not be taking HCQ at baseline.

8. Females who are pregnant or lactating.

9. Uncontrolled infections including and not limited to active bacterial infection
(requiring intravenous [IV] antibiotics at time of initiating study treatment), fungal
infection, human immunodeficiency virus infection with cluster of differentiation 4
(CD4) counts less than 350 and/or AIDS defining opportunistic illnesses known active
hepatitis B [for example, hepatitis B surface antigen positive], patients with
hepatitis C antibody with detectable hepatitis C viral load.. Screening tests are NOT
required for this criterion.

10. The patient has a marked baseline prolongation of QT/QTc interval >470 millisecond
using Fridericia's QT correction formula or a personal history of any of the following
conditions: syncope of cardiovascular etiology, ventricular arrhythmia of pathological
origin (including, but not limited to, ventricular tachycardia and ventricular
fibrillation), sudden cardiac arrest, family history of Long QT syndrome.

11. Patients with symptomatic heart failure, uncontrolled arrhythmia, hypokalemia that
does not respond to supplementation

12. Patient receiving treatment with strong and moderate Cytochrome P450, family 3,
subfamily A (CYP3A) inducers within seven days prior to the first dose of study drugs.

13. Patient receiving treatment with tamoxifen within seven days prior to the first dose
of study drugs.

14. Patient receiving treatment with live vaccines within 30 days prior to the first dose
of study drugs.

15. Patients receiving medications including herbal supplements which may prolong the QT
interval.

Eligibility criteria- Part 2 (Enrollment criteria for the dose-expansion phase)

Inclusion Criteria

1. Postmenopausal women with HR+/ Her2- advanced breast cancer with endocrine naïve
disease will be enrolled in Cohort A. Endocrine naïve patients are defined as advanced
breast cancer patients eligible for first-line aromatase inhibitor in combination with
cyclin-dependent kinase (CDK) 4 / 6 inhibitor therapy. Prior endocrine therapy in the
neoadjuvant or adjuvant setting is permitted if the patient had a disease-free
interval of more than 12 months.

2. Postmenopausal women with HR +/ Her 2 -advanced breast cancer with endocrine
pretreated disease will be enrolled in Cohort B. Endocrine pretreated patients are
defined as advanced breast cancer patients who progressed while receiving endocrine
therapy as first-line therapy or who had prior endocrine therapy in the neoadjuvant or
adjuvant setting with a disease-free interval of less than 12 months and who are
otherwise eligible to receive a combination of Faslodex® and CDK 4 / 6 inhibitor may
be enrolled in Cohort B.

3. Intact G1/S checkpoint in tumor tissue defined by positive-Rb staining and
negative-low-molecule weight isoforms of cyclin E (LMWE) with staining done on
formalin-fixed paraffin embedded slides from archival tissue or cell blocks.

4. Age ≥ 18 years.

5. Men with advanced breast cancer may be enrolled in Cohort A or B if they meet
eligibility criteria as above for post menopausal women.

6. Peri or premenopausal women may be enrolled in Cohort A or B, if they are receiving a
gonadotropin-releasing agonist and meet eligibility criteria as above for
postmenopausal women.

7. Female subjects must meet one of the following:

- Postmenopausal for at least one year before enrollment, OR

- Surgically sterile (i.e., undergone a hysterectomy or bilateral oophorectomy), OR

- If subject is of childbearing potential (defined as not satisfying either of the
above two criteria), agrees to practice two acceptable methods of contraception
(combination methods requires use of two of the following: diaphragm with
spermicide, cervical cap with spermicide, contraceptive sponge, male or female
condom, hormonal contraceptive) from the time of signing of the informed consent
form through 21 days after the last dose of study agent. Patients receiving
Fulvestrant should use effective contraception for one year after last
fulvestrant dose OR o Agree to practice true abstinence when this is in line with
the preferred and usual lifestyle of the subject. (Periodic abstinence [e.g.,
calendar, ovulation, symptothermal, postovulation methods] and withdrawal are not
acceptable contraception methods.)

8. Male subjects, even if surgically sterilized (i.e., status postvasectomy), must agree
to one of the following:

1. Practice effective barrier contraception during the entire study period and
through 60 calendar days after the last dose of study agent, OR

2. Agree to practice true abstinence when this is in line with the preferred and
usual lifestyle of the subject. (Periodic abstinence [e.g., calendar, ovulation,
symptothermal, postovulation methods] and withdrawal are not acceptable
contraception methods.)

9. Patients with asymptomatic CNS metastases not requiring use of corticosteroids will be
allowed

10. Estimated life expectancy of at least six months.

11. ECOG performance status ≤2.

12. Demonstrates measurable disease as defined by RECIST 1.1 criteria or non-measurable
bone-only disease.

13. Documented ophthalmic exam within the last 12 months demonstrating no evidence of
retinopathy. Patients with retinal changes will be considered for enrollment with
written clearance from a board-certified ophthalmologist.

14. Must sign informed consent prior to registration.

15. The patient has adequate organ function for all of the following criteria, as defined
below.

Laboratory Value Guidance to Establish Adequate Organ Function

- Hematologic

- ANC ≥ 1.5 × 109/L

- Platelets ≥100 × 109/L

- Hemoglobin ≥8 g/dL (Patients may receive erythrocyte transfusions to achieve this
hemoglobin level at the discretion of the investigator. Initial treatment must
not begin earlier than the day after the erythrocyte transfusion.)

- Hepatic

- Total bilirubin ≤1.5 × ULN

- Patients with Gilbert's syndrome with a total bilirubin ≤2.0 times ULN and direct
bilirubin within normal limits are permitted.

- ALT and AST ≤3 × ULN

- Renal

- Creatinine Clearance ≥30 mL/minute

16. Patients who previously received chemotherapy must have recovered (Common Terminology
Criteria for Adverse Events (CTCAE) grade ≤1) from the acute effects of chemotherapy
except for residual alopecia or grade 2 peripheral neuropathy prior to randomization.
A washout period of at least 21 days is required between last chemotherapy dose and
first dose of the study drug/s (provided the patient did not receive radiotherapy).

17. Patients who received palliative radiotherapy must have completed and fully recovered
from the acute effects of radiotherapy. A washout period of at least 14 days is
required between end of palliative radiotherapy and first dose of the study drug/s.

18. The patient is able to swallow oral medications.

Exclusion Criteria

1. Presence of visceral crisis, lymphangitic spread, leptomeningeal carcinomatosis or
inflammatory breast cancer.

2. Prior therapy with a CDK 4/6 inhibitor.

3. Serious concomitant systemic disorder that would compromise the safety of the patient
or compromise the patient's ability to complete the study, as determined by the
treating physician or the principal investigator (for example, interstitial lung
disease, severe dyspnea at rest, history of major surgical resection involving the
stomach or small bowel, or preexisting Crohn's disease or ulcerative colitis or a
preexisting chronic condition resulting in baseline grade 2 or higher diarrhea).

4. Second primary malignancy except most in situ carcinoma (e.g., adequately treated
non-melanomatous carcinoma of the skin) or other malignancy treated at least five
years previously with no evidence of recurrence.

5. Uncontrolled or symptomatic CNS metastases.

6. Known history of G6PD deficiency.

7. Taking other commercially available medications which may theoretically either
stimulate or inhibit autophagy; these include calcitriol and chloroquine.

8. Taking medications which may lead to interactions with HCQ, including penicillamine,
telbivudine, botulinum toxin, digoxin, and propafenone.

9. Must not be taking HCQ at baseline.

10. Females who are pregnant or lactating.

11. The patient has active bacterial infection (requiring intravenous [IV] antibiotics at
time of initiating study treatment), fungal infection, or detectable viral infection
(such as known human immunodeficiency virus positivity or with known active hepatitis
B or C [for example, hepatitis B surface antigen positive]). No screening tests is
required for this criterion.

12. The patient has a marked baseline prolongation of QT/QTc interval >470 millisecond
using Fridericia's QT correction formula or a personal history of any of the following
conditions: syncope of cardiovascular etiology, ventricular arrhythmia of pathological
origin (including, but not limited to, ventricular tachycardia and ventricular
fibrillation), or sudden cardiac arrest ,family history of Long QT syndrome.

13. Patients with symptomatic heart failure, uncontrolled arrhythmia, hypokalemia that
does not respond to supplementation

14. Patient receiving treatment with strong and moderate CYP3A inducers within seven days
prior to the first dose of study drugs.

15. Patient receiving treatment with tamoxifen within seven days prior to the first dose
of study drugs.

16. Patient receiving treatment with live vaccines within 30 days prior to the first dose
of study drugs.

17. Patients receiving medications, including herbal supplements, which may prolong the QT
interval.