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Safety, Pharmacokinetics and Efficacy Study of Bisthianostat in Refractory or Recurrent Multiple Myeloma Patients

Phase 1
Conditions
Refractory Multiple Myeloma
Recurrent Multiple Myeloma
Interventions
Registration Number
NCT03618602
Lead Sponsor
Shanghai Theorion Pharmaceutical Co Ltd.
Brief Summary

This is a first-in-human study to investigate the safety, tolerability, pharmacokinetics, and efficacy of Bisthianostat in refractory or recurrent multiple myeloma patients.

Detailed Description

This is a first-in-human, single center, open-label, single arm, dose escalating phase I study. This study will be conducted in 3 parts.

Phase A : Patients will receive single dose of bisthianostat to evaluate the single-dose pharmacokinetics and safety.

Phase B: After single-dose phase, patients will receive multiple dose bisthianostat for 4 weeks on day 1,4,11,14,18,21,25,28 to evaluate the multiple-dose pharmacokinetics and safety

Phase C: Patients will continue on the study if they benefit from the drug and not experience any serious side effects.

Recruitment & Eligibility

Status
UNKNOWN
Sex
All
Target Recruitment
30
Inclusion Criteria
  • Diagnosed as stage II or III (Durie-Salmon Staging System) multiple myeloma with disease progression or recurrence after at least two cycles of systemic antimyeloma treatment.
  • Serum M protein≥ 5.0g / L, or urine M protein ≥ 200mg / 24h, or serum free light chain ≥ 200mg / L.
  • Eastern Cooperative Oncology Group (ECOG) Performance Status of ≤ 2.
  • Expected survival of ≥3 months.
  • Female participants of childbearing potential should have negative urine pregnancy test in screening period (accept previous test result within 14 days before screening), and must agree to adopt effective contraceptive measures within 14 days before receiving first dose of study drug, during the treatment period and within 28 days after final dose of study drug.
  • Male participants must agree to adopt effective contraceptive measures and not allowed to donate sperms during the treatment period, and within 28 days after final dose of study drug.
  • Hemoglobin ≥ 80 g/L, Platelet≥50×109/L (50,000/mm3), Absolute Neutrophil Count≧1.0×109/L (1000 cells/mm3), Prothrombin time(PT) and activated partial thromboplastin time ≤ 2 x Upper Limit of Normal (ULN)
  • AST or ALT ≤ 1.5 x ULN, total bilirubin≤ 1.5 x ULN;
  • Serum Creatinine ≤ 1.5 x ULN, glomerular filtration rate≥ 50 ml/min;
  • NYHA Class I or II
  • Written informed consent obtained prior to participation in the study
Exclusion Criteria
  • Pregnant or lactating women.
  • Non-secretory multiple myeloma patients.
  • Plasma cell leukemia patients.
  • Received any anti-cancer medication or experimental drugs against multiple myeloma within 1 week before first dose of bisthianostat, any experimental treatment other than medication (eg. leukocyte donor/monocyte infusion) within 56 days before first dose of bisthianostat. Participation in any other drug or medical devices within 56 days before the study.
  • Stem cell transplant planned on the following 28 days.
  • Uncontrolled hypercalcemia after treatments, eg. saline infusion.
  • Renal insufficiency required hemodialysis or peritoneal dialysis.
  • NCI-CTCAE grade 2 Peripheral Neuropathy.
  • Serious heart disease in the past 6 months, including angina requiring surgery, uncontrolled hypertension after anti-hypertensive treatments (Systolic blood pressure> 160 mmHg, Diastolic blood pressure>90mmHg); Myocardial infarction; Grade II-IV congestive heart failure; unstable angina.
  • HIV, HCV or HBV (HBV-DNA > 20 IU/mL) infection.
  • Patients with any other prior malignancy, except for skin basal cell carcinoma, cervical carcinoma in situ, breast carcinoma in situ, skin squamous cell carcinoma that have been treated and controlled.
  • Imaging evidences show tumors have involved main blood vessels and nerves.
  • Patients with significant central nervous system lesions.
  • Patients with mental illness.
  • Patients with history of alcohol or drug abuse, patients with allergy to the active ingredient or excipients of study drug, and patients who are unable or unwilling to receive the intravenous administration.
  • Active infection (Bacteria, fungi, virus etc), fever with body temperature > 38 ℃ for reasons unknown.
  • Other situations that investigator considers it's inappropriate for patients to participate in this study.

Study & Design

Study Type
INTERVENTIONAL
Study Design
SEQUENTIAL
Arm && Interventions
GroupInterventionDescription
200mg BisthianostatBisthianostat200mg Bisthianostat taken orally on Day 1, 4,7,11,14,18,21,25 and 28 of each cycle(4 weeks).
100mg BisthianostatBisthianostat100mg starting dose taken orally on Day 1, 4,7,11,14,18,21,25 and 28 of each cycle(4 weeks).
400mg BisthianostatBisthianostat400mg Bisthianostat taken orally on Day 1, 4,7,11,14,18,21,25 and 28 of each cycle(4 weeks).
600mg BisthianostatBisthianostat600mg Bisthianostat taken orally on Day 1, 4,7,11,14,18,21,25 and 28 of each cycle(4 weeks).
Primary Outcome Measures
NameTimeMethod
Maximum tolerated dose of BisthianostatUp to 24 months

To determine the maximum tolerated dose of Bisthianostat in refractory or recurrent multiple myeloma patients.

Treatment-related adverse events considered as dose-limiting toxicityDuring the first cycle (4 weeks)

To evaluate the severity of treatment-related AEs considered as dose-limiting toxicity.

Secondary Outcome Measures
NameTimeMethod
Peak Plasma Concentration (Cmax)During the first cycle (4 weeks)

To determine the Peak Plasma Concentration of Bisthianostat.

Area under the plasma concentration versus time curve (AUC)During the first cycle (4 weeks)

To determine the Area under the plasma concentration versus time curve of Bisthianostat.

Half life (T1/2)During the first cycle (4 weeks)

To determine the half-life of Bisthianostat.

Time of Peak Concentration (Tmax)During the first cycle (4 weeks)

To determine the time of peak concentration of Bisthianostat.

Objective Response RateUp to 1 month after last dose

To evaluate the objective response rate in refractory or recurrent myeloma patients after bisthianostat treatments.

Incidence of adverse events related to treatmentsUp to 1 month after last dose

To evaluate the incidence of adverse events that are related to treatments in refractory or recurrent myeloma patients

Incidence of laboratory abnormalities related to treatmentsUp to 1 month after last dose

To evaluate the incidence of laboratory abnormalities that are related to treatments in refractory or recurrent myeloma patients

Trial Locations

Locations (1)

Renji Hospital

🇨🇳

Shanghai, Shanghai, China

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