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Study of ORIC-101 in Combination With Enzalutamide

Phase 1
Terminated
Conditions
Prostatic Neoplasms
Interventions
Registration Number
NCT04033328
Lead Sponsor
ORIC Pharmaceuticals
Brief Summary

The purpose of this study is to establish the recommended phase 2 dose (RP2D), safety, pharmacokinetics (PK), pharmacodynamics (PD), and preliminary antitumor activity of ORIC-101 in combination with enzalutamide (Xtandi®) when administered to patients with metastatic prostate cancer progressing on enzalutamide.

Detailed Description

ORIC-101 is a small molecule GR antagonist being developed for the treatment of patients with solid tumor malignancies. Mechanistically, ORIC-101 inhibits GR transcriptional activity and blocks the pro-survival signals mediated by the activated nuclear receptor.

This is an open-label, single arm, multicenter, dose escalation followed by dose expansion study to assess the safety and preliminary antitumor activity of ORIC-101 in combination with enzalutamide in patients progressing on enzalutamide. Patients deemed eligible will receive treatment with ORIC-101 in addition to continuing their current enzalutamide therapy.

Escalating dose levels of ORIC-101 will be administered orally, once daily in combination with enzalutamide 160 mg. Parallel enrollment for assessment of PK/PD modulation in up to 3 additional patients presenting with tumors expressing high levels of GR (GR-high) may be performed at each dose level after the dose level has cleared the initial dose-limiting toxicity evaluation period; these additional patients may serve as supplemental patients for selection of the maximum tolerated dose and/or RP2D.

Dose expansion will further evaluate the safety and preliminary antitumor activity of ORIC-101 in patients presenting with different levels of GR expressing-tumors.

Recruitment & Eligibility

Status
TERMINATED
Sex
Male
Target Recruitment
41
Inclusion Criteria
  • Histologically or cytologically confirmed adenocarcinoma of the prostate

  • Metastatic prostate cancer currently being treated with enzalutamide (Xtandi®) 160 mg once daily plus surgical or ongoing chemical castration, with baseline testosterone level <50 ng/dL

  • Must have been on treatment with enzalutamide for at least 3 months prior to documented evidence of PSA progression defined as per PCWG3: minimum of 2 rising values (3 measurements) obtained a minimum of one week apart with the latest result being at least 2.0 ng/mL (or 1.0 ng/mL if PSA rise is the only indication of progression)

  • Agreement and ability to undergo on-study core biopsies, as follows, through a procedure that is deemed to be clinically feasible and not carry significant risk:

    • one pre-treatment tumor biopsy obtained while on treatment with enzalutamide prior to enrollment on this study; and
    • one post-treatment tumor biopsy during Cycle 2
    • one end of treatment tumor biopsy (optional)
  • ECOG performance status 0 or 1

  • Life expectancy of at least 3 months

  • Adequate organ function as defined by the following criteria:

    • ANC ≥1500 cells/mm3 (1.5 × 103 cells/mm3)
    • Platelets ≥100,000 /µL (100 × 109 /L)
    • Hemoglobin ≥9.0 g/dL (90 g/L)
    • AST (SGOT) or ALT (SGPT) ≤2.5 × ULN, ≤5.0 × ULN for patients with liver metastases
    • Bilirubin ≤1.5 × ULN; patients with a known history of Gilbert's syndrome and/or isolated elevations of indirect bilirubin are eligible
    • QTcF ≤480 msec
  • Capable of giving signed informed consent

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Exclusion Criteria
  • No intervening therapy between enzalutamide treatment and enrollment on this study
  • Any other active malignancy, with the exception of adequately treated non-melanoma skin cancer, adequately treated superficial bladder cancer, stage 1 or 2 solid tumor malignancies without evidence of disease, or other solid tumors curatively treated with no evidence of disease for ≥5 years from enrollment
  • Current treatment on another therapeutic clinical trial
  • Prior or current treatment with ORIC-101 or any other GR antagonist (eg, CORT-125281, mifepristone, relacorilant)
  • Prior chemotherapy in the metastatic castration-resistant prostate cancer setting
  • Prior treatment with a second-generation AR modulator (eg, apalutamide, abiraterone, darolutamide)
  • History of Cushing's syndrome or adrenal insufficiency
  • History or presence of CNS metastases
  • History of seizures or condition that may predispose to seizures
  • Current (at C1D1) or requirement for chronic use of systemic corticosteroids with the exception of inhaled, topical, intraocular, intranasal, or intraarticular corticosteroids
  • Current (within 10 days prior to first dose of ORIC-101) or expected on-study treatment with specified strong CYP3A4 inhibitors or inducers
  • Receiving any other anticancer therapy, including radiotherapy within 21 days prior to C1D1. Patients must have recovered from all toxicities from prior anticancer therapies and/or radiotherapy
  • Major surgery within 21 days prior to C1D1 or incomplete recovery from adverse effects resulting from such procedure
  • Known human immunodeficiency virus (HIV) infection, unless patient is healthy and has a low risk of AIDS-related outcomes
  • Active Hepatitis B or C infection
  • Any other condition or circumstance (eg, clinical, psychological, familial, sociological, inability to swallow oral study drug) that, in the opinion of the investigator, may interfere with protocol compliance or contraindicates participation in the study
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Study & Design

Study Type
INTERVENTIONAL
Study Design
SEQUENTIAL
Arm && Interventions
GroupInterventionDescription
Dose Escalationenzalutamide 40 MG oral capsule [Xtandi]ORIC-101 dosed orally, once per day in combination with enzalutamide (160 mg) of each 28-day cycle.
Dose ExpansionORIC-101RP2D dose
Dose EscalationORIC-101ORIC-101 dosed orally, once per day in combination with enzalutamide (160 mg) of each 28-day cycle.
Dose Expansionenzalutamide 40 MG oral capsule [Xtandi]RP2D dose
Primary Outcome Measures
NameTimeMethod
Recommended Phase 2 Dose (RP2D)12 months

RP2D as determined by 3+3 dose escalation design

Number of Participants with Adverse Events36 months

Safety and tolerability of ORIC-101 in combination with enzalutamide

PSA Progression36 months

From study start until PCWG3 criteria is met

Number of Participants with Abnormal 12-lead ECG36 months

Safety and tolerability of ORIC-101 in combination with enzalutamide

PSA Response Rate36 months

≥50% decline from baseline at 8 weeks per Prostate Cancer Working Group 3 (PCWG3) criteria

Number of Participants with Abnormal Laboratory Values36 months

Safety and tolerability of ORIC-101 in combination with enzalutamide

Number of Participants with Abnormal Vital Signs36 months

Safety and tolerability of ORIC-101 in combination with enzalutamide

Secondary Outcome Measures
NameTimeMethod
Overall survival (OS)36 months

Time from first dose to death

Circulating tumor cells (CTCs) conversion36 months

≥5 cells/7.5 mL of blood to 0 (zero) (CTC0), as well as from unfavorable (≥5 cells/7.5 mL of blood) to favorable (\<5 cells/7.5 mL of blood)

Minimum plasma concentration (Cmin)36 months

PK of ORIC-101 in combination with enzalutamide

Time of maximum observed concentration (Tmax)28 Days

PK of ORIC-101 in combination with enzalutamide

Maximum plasma concentration (Cmax)28 Days

PK of ORIC-101 in combination with enzalutamide

Area under the curve (AUC(0-24))28 Days

PK of ORIC-101 in combination with enzalutamide

Elimination half-life (T1/2)28 Days

PK of ORIC-101 in combination with enzalutamide

Objective response rate (ORR)36 months

Response Evaluation Criteria in Solid Tumors (RECIST) v1.1 and PCWG3 criteria

Duration of response (DOR)36 months

Radiographic progression using RECIST v1.1

Progression-free survival (PFS)36 months

Time from first dose to first documentation of radiographic progression or death

Number of Participants with GR Expression by IHC36 months

Level of GR expression by IHC in tumor tissue samples

Trial Locations

Locations (3)

Carolina Urologic Research Center

🇺🇸

Myrtle Beach, South Carolina, United States

MD Anderson Cancer Center

🇺🇸

Houston, Texas, United States

Memorial Sloan Kettering Cancer Center

🇺🇸

New York, New York, United States

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