An Early Phase 1 interventional study of isoquercetin or quercetin in Healthy, sponsored by Beth Israel Deaconess Medical Center. Completed at 1 site in United States. Open to participants aged 18 Years to 80 Years, including healthy volunteers. Per ClinicalTrials.gov, last updated 2020-10-12.
Sponsored by Beth Israel Deaconess Medical Center · Early Phase 1, Interventional, and Basic science
The goal of this study is to evaluate how much quercetin or isoquercetin is absorbed after a single dose and evaluate for pharmacokinetic inhibition of protein disulfide isomerase. Pharmacodynamic studies will also be performed in an additional cohort of 10 patients with evidence of antiphospholipid antibodies
To compare the absorption and activity of quercetin or isoquercetin with or without ascorbic acid in healthy adults. Oral chews containing quercetin (500mg) or isoquercetin(500 mg total) with or without ascorbic acid will be given. Pharmacokinetic parameters (AUC, Cmax, Tmax, elimination half-life) will be determined over 24 hours (8 time points). Pharmacodynamic inhibition of protein disulfide isomerase activity will also be assessed.
In addition to healthy subjects, a cohort of 10 individuals with antiphospholipid antibodies will participate. These participants will receive isoquercetin 1000 mg and have pharmacodynamics studies performed at time 0 and 4 hours.
All study drugs will be provided by Quercegen Pharma.
75 studies on the registry are indexed under Thrombophilia; 16 are open to participants now.
This study's enrollment of 38 is below the median of 86 across 23 interventional studies indexed under Thrombophilia.
Browse Thrombophilia studies →Beth Israel Deaconess Medical Center is the lead sponsor of 560 studies on the registry; 80 are open to participants now.
Of its 75 completed or terminated interventional studies of FDA-regulated products, 61 (81%) have results posted.
Counted across the registry records on this site, refreshed daily.
Subjects in group D must exhibit good organ reserves (within prior 4 weeks) defined as:
Exclusion Criteria
Currently taking aspirin, NSAIDS, warfarin, low-molecular weight heparin or other anticoagulants (such as direct thrombin inhibitors or factor X inhibitors)
a. Note: Study subjects taking aspirin or NSAIDS, if treating physician concurs, are permitted to enroll if plan to hold for aspirin 10 days or NSAIDS 24 hours prior to dosing of quercetin/isoquercetin
Single dose of quercetin with or without ascorbic acid
Drug: isoquercetin or quercetin
Single dose of isoquercetin with or without ascorbic acid
Drug: isoquercetin or quercetin
Single dose PK/PD study
AUC
AUC 0-24 hours of measured plasma quercetin aglycone for Arms A1, B1, A2, B2, C Collected at timepoints: baseline and 1, 2, 4, 6, 8, and 24 hours after dose. PK and PDI samples were not measured for Arm D (anti-phospholipid antibody cohort)
Time frame: 24 hours
Reductase Activity of PDI Using Dieosin Glutathione Disulfide
Measurement of protein disulfide inhibition in plasma using a fluorescent PDI substrate (dieosin glutathione disulfide)
Time frame: 2 hours. Not measured in D
Platelet-induced Thrombin Generation (U/mL)
Thrombin induced thrombin generation measured in patient plasma
Time frame: 4 hours
| Milestone | Quercetin 500mg (ARM A1) | Isoquercetin 500mg (ARM B1) | Quercetin 500 mg + Ascorbic Acid (ARM A2) | Isoquercetin 500 mg + Ascorbic Acid (ARM B2) | Isoquercetin 1000 mg + Ascorbic Acid (ARM C) | Antiphospholipid Antibody Cohort (ARM D) |
|---|---|---|---|---|---|---|
| Started | 5 | 5 | 5 | 5 | 10 | 8 |
| Completed | 5 | 5 | 5 | 5 | 10 | 6 |
| Not completed | 0 | 0 | 0 | 0 | 0 | 2 |
| Withdrew: Withdrawal by subject | 0 | 0 | 0 | 0 | 0 | 2 |
AUC 0-24 hours of measured plasma quercetin aglycone for Arms A1, B1, A2, B2, C Collected at timepoints: baseline and 1, 2, 4, 6, 8, and 24 hours after dose. PK and PDI samples were not measured for Arm D (anti-phospholipid antibody cohort)
| uM hr/L | Quercetin 500 mg (ARM A1) | Isoquercetin 500 mg (ARM B1) | Quercetin 500 mg + Ascorbic Acid (ARM A2) | Isoquercetin 500 mg + Ascorbic Acid (ARM B2) | Isoquercetin 1000 mg + Ascorbic Acid (ARM C) |
|---|---|---|---|---|---|
| AUC | 4.78 ± 1.67 | 15.00 ± 8.94 | 5.41 ± 2.13 | 16.34 ± 10.08 | 40.3 ± 17.11 |
Measurement of protein disulfide inhibition in plasma using a fluorescent PDI substrate (dieosin glutathione disulfide)
| Percent inhibition | Quercetin 500 mg (ARM A1) | Isoquercetin 500 mg (ARM B1) | Quercetin 500 mg + Ascorbic Acid (ARM A2) | Isoquercetin 500 mg + Ascorbic Acid (ARM B2) | Isoquercetin 1000 mg + Ascorbic Acid (ARM C) |
|---|---|---|---|---|---|
| Reductase Activity of PDI Using Dieosin Glutathione Disulfide | 31.9 ± 24.14 | 63.2 ± 25.3 | 16 ± 31.8 | 8.3 ± 15.03 | 38 ± 35 |
Thrombin induced thrombin generation measured in patient plasma
| U/mL | Isoquercetin 1000 mg + Ascorbic Acid (ARM C) | Antiphospholipid Antibody (ARM D) |
|---|---|---|
| Platelet-induced Thrombin Generation (U/mL) | 0.30 ± .28 | 1.40 ± 2.14 |
Collected over Assessed during visit 1, up to 24 hours. Non-serious events are listed at a 0% frequency threshold.
| Group | Deaths | Serious | Other |
|---|---|---|---|
| Quercetin 500 mg (ARM A1) | 0/5 (0%) | 0/5 (0%) | 0/5 (0%) |
| Isoquercetin 500 mg (ARM B1) | 0/5 (0%) | 0/5 (0%) | 0/5 (0%) |
| Quercetin 500 mg + Ascorbic Acid (ARM A2) | 0/5 (0%) | 0/5 (0%) | 0/5 (0%) |
| Isoquercetin 500 mg + Ascorbic Acid (ARM B2) | 0/5 (0%) | 0/5 (0%) | 0/5 (0%) |
| Isoquercetin 1000 mg + Ascorbic Acid (ARM C) | 0/10 (0%) | 0/10 (0%) | 0/10 (0%) |
| Antiphospholipid Antibody (ARM D) | 0/6 (0%) | 0/6 (0%) | 0/6 (0%) |
Measure Analysis Population Description: Antiphospholipid Antibody (ARM D): 2 withdrew consent without any data collected
| Age, Categorical(Participants) | Quercetin 500 mg (ARM A1) | Isoquercetin 500 mg (ARM B1) | Quercetin 500 mg + Ascorbic Acid (ARM A2) | Isoquercetin 500 mg + Ascorbic Acid (ARM B2) | Isoquercetin 1000 mg + Ascorbic Acid (ARM C) | Antiphospholipid Antibody (ARM D) | Total |
|---|---|---|---|---|---|---|---|
| <=18 years | 0 | 0 | 0 | 0 | 0 | 0 | 0 |
| Between 18 and 65 years | 5 | 5 | 5 | 5 | 10 | 4 | 34 |
| >=65 years | 0 | 0 | 0 | 0 | 0 | 2 | 2 |
| Sex: Female, Male(Participants) | Quercetin 500 mg (ARM A1) | Isoquercetin 500 mg (ARM B1) | Quercetin 500 mg + Ascorbic Acid (ARM A2) | Isoquercetin 500 mg + Ascorbic Acid (ARM B2) | Isoquercetin 1000 mg + Ascorbic Acid (ARM C) | Antiphospholipid Antibody (ARM D) | Total |
|---|---|---|---|---|---|---|---|
| Female | 2 | 3 | 2 | 3 | 5 | 5 | 20 |
| Male | 3 | 2 | 3 | 2 | 5 | 1 | 16 |
| Ethnicity (NIH/OMB)(Participants) | Quercetin 500 mg (ARM A1) | Isoquercetin 500 mg (ARM B1) | Quercetin 500 mg + Ascorbic Acid (ARM A2) | Isoquercetin 500 mg + Ascorbic Acid (ARM B2) | Isoquercetin 1000 mg + Ascorbic Acid (ARM C) | Antiphospholipid Antibody (ARM D) | Total |
|---|---|---|---|---|---|---|---|
| Hispanic or Latino | 0 | 0 | 0 | 0 | 2 | 0 | 2 |
| Not Hispanic or Latino | 2 | 1 | 2 | 1 | 5 | 6 | 17 |
| Unknown or Not Reported | 3 | 4 | 3 | 4 | 3 | 0 | 17 |
| Race (NIH/OMB)(Participants) | Quercetin 500 mg (ARM A1) | Isoquercetin 500 mg (ARM B1) | Quercetin 500 mg + Ascorbic Acid (ARM A2) | Isoquercetin 500 mg + Ascorbic Acid (ARM B2) | Isoquercetin 1000 mg + Ascorbic Acid (ARM C) | Antiphospholipid Antibody (ARM D) | Total |
|---|---|---|---|---|---|---|---|
| American Indian or Alaska Native | 0 | 0 | 0 | 0 | 0 | 0 | 0 |
| Asian | 1 | 1 | 1 | 1 | 1 | 0 | 5 |
| Native Hawaiian or Other Pacific Islander | 0 | 0 | 0 | 0 | 0 | 0 | 0 |
| Black or African American | 1 | 0 | 1 | 0 | 0 | 1 | 3 |
| White | 2 | 2 | 2 | 2 | 5 | 5 | 18 |
| More than one race | 0 | 0 | 0 | 0 | 0 | 0 | 0 |
| Unknown or Not Reported | 1 | 2 | 1 | 2 | 4 | 0 | 10 |
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Plan to share: Yes — Contact PI
Supporting information: Study protocol
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Beth Israel Deaconess Medical Center