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BOLD-100 in Combination with FOLFOX for the Treatment of Advanced Solid Tumours

B

Bold Therapeutics

Status and phase

Enrolling
Phase 2
Phase 1

Conditions

Cholangiocarcinoma
Gastric Cancers
Pancreatic Cancer
Colorectal Cancer

Treatments

Drug: BOLD-100 in combination with FOLFOX Chemotherapy (Dose Expansion)
Drug: BOLD-100 in combination with FOLFOX Chemotherapy (Dose Escalation)

Study type

Interventional

Funder types

Industry

Identifiers

NCT04421820
BOLD-100-001

Details and patient eligibility

About

BOLD-100 is an intravenously administered sterile solution containing the ruthenium-based small molecule. BOLD-100 has been shown to preferentially decrease the expression of GRP78 in tumour cells and ER stressed cells when compared to normal cells. BOLD-100 will be combined with cytotoxic FOLFOX chemotherapy in this study, with a dose escalation cohort to ensure tolerability and safety, followed by a cohort expansion phase.

Enrollment

220 estimated patients

Sex

All

Ages

18+ years old

Volunteers

No Healthy Volunteers

Inclusion criteria

  1. Be 18 years or older.

  2. Be male or non-pregnant females who agree to comply with applicable contraceptive requirements of the protocol (see Table 12. Acceptable Contraceptive Methods.)

  3. Histologically and/or cytologically confirmed gastrointestinal tumours that are metastatic or unresectable, and are subject to receive FOLFOX as SOC per investigator's judgement. Participants will have received at least one line of chemotherapy in the metastatic setting. Colorectal cancer: Patients must have received at least 1 prior line of therapy prior to enrollment in this study. Pancreatic cancer: Patients must have received at least 1 prior line of therapy. Gastric cancer: Patients who have not received prior treatment may be included in this study. GEJ (gastroesophageal junction) cancer patients are considered eligible to enter this trial. Cholangiocarcinoma: locally advanced or metastatic biliary tract cancer (intra or extrahepatic cholangiocarcinoma or gallbladder cancer) are eligible to enter this trial. Patients must have received at least 1 prior line of therapy (with gemcitabine-based chemotherapy). Colorectal cancer (ARM VI): Patients must have received at least 2 prior lines of therapy prior to enrollment in this study, one of which was a 5-FU based regimen. Colorectal cancer (ARM VII): Patients must have received only 1 prior line of therapy in the metastatic setting but remain naïve to oxaliplatin prior to enrollment in this study.

  4. Have measurable disease according to RECIST v1.1 (at least one measurable lesion).

  5. Have an anticipated survival of at least 16 weeks.

  6. Be ambulatory, with an Eastern Cooperative Oncology Group (ECOG) performance score of 0 or 1.

  7. Have adequate organ function, defined as:

    1. Hematologic: ANC ≥ 1.5 x 109/L, Hgb ≥ 9.0 g/dL and platelet count ≥ 100 x 109/L
    2. Hepatic: total bilirubin ≤ 1.5 x ULN (or ≤ 3 x ULN for subjects with Gilbert's Syndrome); transaminases ≤ 2.5 x ULN (may be up to ≤ 5x ULN if clearly due to liver metastases) and ALP ≤ 2.5 x ULN (or ≤ 3 x ULN if liver metastases).
    3. Renal: serum creatinine ≤ 1.5 x ULN or creatinine clearance ≥ 50 mL/min.

    c. Urine protein is 0, trace, or +1 on dipstick urinalysis, or < 1.0 gram on 24-hour urine protein analysis

  8. Be on stable doses of any drugs that may affect hepatic drug metabolism or renal drug excretion (e.g., non-steroidal anti-inflammatory drugs, corticosteroids, barbiturates, diphenylhydantoin, narcotic analgesics, probenecid). Such drugs should not be initiated while the subject is participating in this study or have been initiated within 30 days beforehand before the start of treatment. Whenever possible, narcotic analgesic doses should be stable within 30 days prior to study entry and during the first cycle of therapy.

  9. Resolved acute effects of any prior therapy before the start of treatment to baseline severity or grade ≤1 CTCAE 5.0 except for adverse events not constituting a safety risk by investigator judgment (such as alopecia)

  10. Able to take oral medications (for pre-medications and supportive management)

  11. Understand and be able, willing, and likely to fully comply with study procedures and restrictions.

  12. Be fully informed about their illness and the investigational nature of the study protocol, and sign a REB-approved Informed Consent Form (ICF).

  13. (ARM VII): BRAF wild-type tumour status

Exclusion criteria

  1. Neuropathy > grade 2

  2. Previous intolerance to or significant reaction secondary to fluorouracil or oxaliplatin

  3. Cerebrovascular accident within the past 6 months before the start of treatment.

  4. History or presence of central nervous system (CNS) metastasis or leptomeningeal tumours as documented by CT or MRI scan, analysis of cerebrospinal fluid or neurological exam.

  5. Any serious medical conditions that might be aggravated by treatment or limit compliance. This includes, but is not limited to uncontrolled psychiatric disorders, serious infections, active peptic ulcer disease and bleeding diathesis

  6. Any history of serious cardiac illness including (but not confined to):

    • Previous or active myocardial infarction < 6 months before the start of treatment
    • Congestive cardiac failure (NYHA III or IV)
    • History of unstable angina pectoris < 6 months before the start of treatment
    • Recent coronary artery bypass grafting < 6 months before the start of treatment
    • Uncontrolled hypertension (systolic ≥ 140 mmHg or diastolic ≥ 90 mmHg)
    • Ventricular arrhythmia < 6 months before the start of treatment
    • Left ventricular ejection fraction (LVEF) < 50% as measured either by radionuclide angiography or echocardiogram
    • QTc interval > 470 msec
  7. Hemoptysis, cerebral, or clinically significant gastrointestinal hemorrhage in the past 6 months before the start of treatment

  8. Any other known malignancy within 3 years before the start of treatment (with the exception of non-melanoma skin cancer that had undergone curative treatment, cervical cancer in situ, or ductal/lobular carcinoma in situ of the breast that has underwent local treatment

  9. Active gastrointestinal tract disease with malabsorption syndrome.

  10. Non-healing wound, fracture, or ulcer, or presence of symptomatic peripheral vascular disease.

  11. Treatment with radiation therapy or surgery within 4 weeks prior to starting treatment.

  12. Recent history of weight loss > 10% of current body weight in past 3 months before the start of treatment.

  13. Current (within 1 week of the start of the study) or regular use of any medication (including OTC, herbal or homeopathic preparations) that could affect (improve or worsen) the cancer being studied, or could affect the action or disposition of BOLD-100, or its clinical or laboratory assessment, e.g., Coumadin therapy, due to high competitive protein binding.

  14. HIV-positive subjects on combination anti-retroviral therapy due to the potential for PK interactions with the study agent.

  15. Any condition potentially decreasing compliance to study procedures. Concurrent use of another investigational therapy or anti-cancer therapy.

  16. Concurrent use of another investigational therapy or anti-cancer therapy within 4 weeks before the start of treatment.

  17. Currently breastfeeding

  18. Dihydropyrimidine Dehydrogenase (DPD) deficiency

  19. Current or prior treatment with potent inhibitors of Dihydropyrimidine Dehydrogenase (DPD)

  20. (ARM VII): Prior oxaliplatin treatment in the 1st line setting

  21. (ARM VII): Prior exposure to BOLD-100

  22. (ARM VII): Subjects with microsatellite-high (MSI-H) Tumours

  23. (ARM VII): Concurrent monoclonal antibody therapy for mCRC (anti-EGFR, anti-VEGF or anti-HER2)

Trial design

Primary purpose

Treatment

Allocation

Non-Randomized

Interventional model

Single Group Assignment

Masking

None (Open label)

220 participants in 11 patient groups

Part B - Dose Expansion - 1L Gastric Cancer (ARM I)
Experimental group
Description:
Arm closed to enrollment.
Treatment:
Drug: BOLD-100 in combination with FOLFOX Chemotherapy (Dose Expansion)
Part B - Dose Expansion - 2L Gastric Cancer (ARM II)
Experimental group
Description:
Arm closed to enrollment.
Treatment:
Drug: BOLD-100 in combination with FOLFOX Chemotherapy (Dose Expansion)
Part B - Dose Expansion - 2L Pancreatic Cancer (ARM III)
Experimental group
Description:
Arm closed to enrollment.
Treatment:
Drug: BOLD-100 in combination with FOLFOX Chemotherapy (Dose Expansion)
Part B - Dose Expansion - 2L Colorectal Cancer (ARM IV)
Experimental group
Description:
Arm closed to enrollment.
Treatment:
Drug: BOLD-100 in combination with FOLFOX Chemotherapy (Dose Expansion)
Part B - Dose Expansion - 3L Colorectal Cancer (ARM VI)
Experimental group
Description:
Arm closed to enrollment.
Treatment:
Drug: BOLD-100 in combination with FOLFOX Chemotherapy (Dose Expansion)
Part B - Dose Expansion - 2L Cholangiocarcinoma (ARM V)
Experimental group
Description:
Arm closed to enrollment.
Treatment:
Drug: BOLD-100 in combination with FOLFOX Chemotherapy (Dose Expansion)
Part A - Dose Escalation - Gastric Cancer
Experimental group
Description:
Arm closed to enrollment.
Treatment:
Drug: BOLD-100 in combination with FOLFOX Chemotherapy (Dose Escalation)
Part A - Dose Escalation - Pancreatic Cancer
Experimental group
Description:
Arm closed to enrollment.
Treatment:
Drug: BOLD-100 in combination with FOLFOX Chemotherapy (Dose Escalation)
Part A - Dose Escalation - Colorectal Cancer
Experimental group
Description:
Arm closed to enrollment.
Treatment:
Drug: BOLD-100 in combination with FOLFOX Chemotherapy (Dose Escalation)
Part A - Dose Escalation - Cholangiocarcinoma
Experimental group
Description:
Arm closed to enrollment.
Treatment:
Drug: BOLD-100 in combination with FOLFOX Chemotherapy (Dose Escalation)
Part B - Dose Expansion - 2L Colorectal Cancer (ARM VII) - Randomized
Active Comparator group
Description:
Arm open to enrollment.
Treatment:
Drug: BOLD-100 in combination with FOLFOX Chemotherapy (Dose Expansion)

Trial contacts and locations

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Central trial contact

Jim Pankovich; Michelle Jones

Data sourced from clinicaltrials.gov

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