Status:

TERMINATED

Study of XL102 as Single-Agent and Combination Therapy in Subjects With Solid Tumors (QUARTZ-101)

Lead Sponsor:

Exelixis

Conditions:

Neoplasm Malignant

Epithelial Ovarian Cancer

Eligibility:

All Genders

18+ years

Phase:

PHASE1

Brief Summary

This is a Phase 1, open-label, dose-escalation and expansion study evaluating the safety, tolerability, PK, antitumor activity, and effect on biomarkers of XL102 administered orally alone and in multi...

Eligibility Criteria

Inclusion

  • Cytologically or histologically and radiologically confirmed solid tumor that is inoperable, locally advanced, metastatic, or recurrent.
  • Dose-Escalation Stage Cohort A (Solid Tumors): The subject has a solid tumor that is unresectable or metastatic and for which life-prolonging measures do not exist or available therapies are intolerable or no longer effective.
  • Dose-Escalation Stage Cohort B and Cohort-Expansion Stage Cohorts F and H (Hormone Receptor-Positive Breast Cancer): Subjects with breast cancer that is hormone receptor-positive (estrogen receptor positive \[ER+\] and/or progesterone receptor positive \[PR+\]) and negative for human epidermal growth factor receptor 2 (HER-2 negative \[HER-2-\]) and who have documented radiographic disease progression during or following their last systemic anticancer therapy for inoperable locally advanced or metastatic disease.
  • Dose-Escalation Stage Cohort C and Cohort-Expansion Stage Cohorts G and I (Metastatic Castration-Resistant Prostate Cancer): Subjects with adenocarcinoma of the prostate. Note: Neuroendocrine differentiation and other histological features are permitted if adenocarcinoma is the primary histology.
  • Cohort-Expansion Stage Cohort D (Triple Negative Breast Cancer): Subjects with breast cancer that is negative for HER-2, estrogen receptors, and progesterone receptors, and who have documented radiographic disease progression during or following their last systemic anticancer therapy for inoperable locally advanced or metastatic disease.
  • Cohort-Expansion Stage Cohort E (Epithelial Ovarian Cancer): Subjects with epithelial ovarian cancer, including primary peritoneal cancer (PPC) and fallopian tube cancer (FTC) who have platinum-resistant disease following treatment with a platinum-containing chemotherapy. Ovarian borderline epithelial tumors (low malignant potential) are excluded.
  • Expansion Cohorts: Subjects must have measurable disease per RECIST 1.1 as determined by the Investigator.
  • Tumor tissue material (archival or fresh tumor tissue \[if it can be safely obtained\]).
  • Recovery to baseline or ≤ Grade 1 severity (Common Terminology Criteria for Adverse Events version 5 \[CTCAE v5\]) from AEs, unless AEs are clinically nonsignificant (eg, alopecia) or stable (eg, peripheral neuropathy).
  • Eastern Cooperative Oncology Group (ECOG) Performance Status of 0-1.
  • Adequate organ and marrow function.
  • Sexually active fertile subjects and their partners must agree to use medically accepted methods of contraception.
  • Female subjects of childbearing potential must not be pregnant at screening.

Exclusion

  • Receipt of XL102 or any other selective CDK7 inhibitor.
  • Receipt of any cytotoxic chemotherapy therapy or anticancer antibody therapy within 21 days before first dose of study treatment.
  • Receipt of any type of small molecule kinase inhibitor within 2 weeks before first dose of study treatment.
  • Receipt of any anticancer hormonal therapy within 2 weeks or within 5 half-lives of the agent, whichever is shorter, before first dose of study treatment. HR+BC subjects enrolled in the Combination Cohorts B and H receiving fulvestrant prior to first dose of study treatment are allowed to continue with their fulvestrant treatment. Metastatic CRPC subjects enrolled in the Combination Cohorts C and I receiving abiraterone prior to first dose of study treatment are allowed to continue with their abiraterone treatment.
  • Radiation therapy within 14 days before first dose of study treatment. Subjects with clinically relevant ongoing complications from prior radiation therapy are not eligible.
  • Known brain tumors and metastases or cranial epidural disease unless adequately treated with radiotherapy and/or surgery (including radiosurgery) and stable for at least 4 weeks before first dose of study treatment.
  • Use of strong inhibitors or inducers of cytochrome P450 (CYP) 3A4, and inhibitors of P-glycoprotein (P-gp) or breast cancer resistance protein (BCRP) transporter within 5 half-lives or 4 weeks prior to first dose of study treatment, whichever is shorter.
  • Use of a sensitive substrate of CYP3A4, CYP2B6, CYP2C8, CYP2C9, or BCRP transporter within 5 half-lives or 4 weeks prior to first dose of study treatment, whichever is shorter. For subjects with mCRPC in receiving combination treatment with XL102 and abiraterone plus prednisone, use of a substrate of CYP2D6 with a narrow therapeutic index within 5 half-lives or 4 weeks prior to first dose of study treatment, whichever is shorter, is prohibited.
  • The subject has uncontrolled, significant intercurrent or recent illness including, but not limited to, the following conditions:
  • Cardiovascular disorders: i. congestive heart failure New York Heart Association class 3 or 4, unstable angina pectoris, serious cardiac arrhythmias (eg, ventricular flutter, ventricular fibrillation, torsades de pointes). ii. uncontrolled hypertension defined as sustained blood pressure \> 150 mmHg systolic or \>90 mm Hg diastolic despite optimal antihypertensive treatment. iii. stroke (including transient ischemic attack \[TIA\]), myocardial infarction, or other ischemic event or pulmonary embolism (PE) within 6 months before first dose. Note: Subjects with a diagnosis of deep vein thrombosis (DVT) within 6 months before first dose are allowed if managed adequately with anticoagulants and asymptomatic at the time of first dose.
  • history of any lower gastrointestinal (GI) disorder (such as inflammatory bowel disease \[IBD\]) or any form of colitis (such as ulcerative colitis or Crohn's disease).
  • history of upper gastrointestinal (GI) inflammatory disorder (eg, esophagitis, gastritis, or duodenitis), gastroparesis, symptomatic gastroesophageal reflux disease (GERD) despite medical therapy, or gastric or duodenal ulcers within 6 months.
  • history of major surgical resection involving the stomach or small bowel or any other reason for a malabsorption syndrome.
  • history of significant bleeding (eg, GI hemorrhage) within 12 weeks before first dose.
  • active infection requiring systemic treatment, infection with human immunodeficiency virus (HIV) or acquired immunodeficiency syndrome (AIDS)-related illness, acute or chronic hepatitis B or C infection, or a known positive test for tuberculosis infection if supported by clinical or radiographic evidence of disease. Prophylactic use of antibiotics is allowed.
  • History of COVID-19 unless the subject has clinically recovered from the infection: at least 10 days prior to first dose or sooner, if COVID-19 PCR negative.
  • moderate to severe hepatic impairment (child-pugh B or C)
  • requirement for hemodialysis or peritoneal dialysis
  • history of solid organ, autologous or allogenic stem cell transplant
  • Concomitant use of certain medications.
  • Uncontrolled, significant intercurrent or recent illness.
  • Major surgery within 4 week before first dose of treatment. Minor surgery within 7 days before first dose of treatment. Complete wound healing from surgery must have occurred before first dose of treatment.
  • Corrected QT interval calculated by the Fridericia formula (QTcF) \> 480 ms per electrocardiogram (ECG).
  • History of psychiatric illness likely to interfere with ability to comply with protocol requirements or give informed consent.
  • Inability to swallow oral study treatment formulation
  • Previously identified allergy or hypersensitivity to study treatment formulation
  • Pregnant or lactating females.
  • Diagnosis of another malignancy within 2 years before first dose of study treatment, except for superficial skin cancers, or localized, low grade tumors deemed cured and not treated with systemic therapy.
  • For subjects in Food-Effect Cohorts (A-FE) only: i. Known inability to tolerate high-fat meal provided on Day 1 ii. Allergy to meal components or dietary restrictions iii. Unable to fast for 4 hours predose and 2 hours post dose on Day 8

Key Trial Info

Start Date :

February 10 2021

Trial Type :

INTERVENTIONAL

Allocation :

ACTUAL

End Date :

May 2 2024

Estimated Enrollment :

52 Patients enrolled

Trial Details

Trial ID

NCT04726332

Start Date

February 10 2021

End Date

May 2 2024

Last Update

May 14 2024

Active Locations (5)

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Page 1 of 2 (5 locations)

1

Exelixis Clinical Site #4

Atlanta, Georgia, United States, 30322

2

Exelixis Clinical Site #3

Boston, Massachusetts, United States, 02215

3

Exelixis Clinical Site #2

Dallas, Texas, United States, 75230

4

Exelixis Clinical Site #5

Houston, Texas, United States, 77030

Study of XL102 as Single-Agent and Combination Therapy in Subjects With Solid Tumors (QUARTZ-101) | DecenTrialz