Phase 1
Completed N=70
A Study to Assess the Safety and Tolerability of Single and Multiple Ascending Doses of Oral RO7020531 in Chinese Healthy Participants.
Healthy Participants
Source: ClinicalTrials.gov NCT03530917 ↗
Enrolled (actual)
70
Serious AEs
1.4%
Results posted
Jul 2020
Primary outcomePrimary: Percentage of Participants With Adverse Events (AEs) — 37.5; 37.5; 25.0; 50.0 Percentage of Participants
Summary
To evaluate the safety and tolerability of single and multiple ascending doses of oral RO7020531 in Chinese healthy participants.
Outcome Measures
| Outcome | Result | p-value |
|---|---|---|
| PRIMARY Percentage of Participants With Adverse Events (AEs) |
37.5; 37.5; 25.0; 50.0; 100; 100 | — |
| SECONDARY Maximum Observed Plasma Concentration (Cmax) for RO7020531, Main Active Metabolite (RO7011785) and Prodrug Metabolites (RO7018822 and RO7033805) |
NA; NA; 0.14; NA; 1.08; 1.56 | — |
| SECONDARY Area Under the Plasma Concentration Versus Time Curve up to the Last Measurable Concentration (AUClast) for RO7020531, Main Active Metabolite (RO7011785) and Prodrug Metabolites (RO7018822 and RO7033805) |
0.00; 0.00; 0.02; 0.00; 0.14; 0.92 | — |
| SECONDARY Area Under the Plasma Concentration Versus Time Curve Extrapolated to Infinity (AUCinf) for RO7020531, Main Active Metabolite (RO7011785) and Prodrug Metabolites (RO7018822 and RO7033805) |
714; 1670; 2510; 2720; 1880; 2660 | — |
| SECONDARY Time to Maximum Observed Plasma Concentration (Tmax) for RO7020531, Main Active Metabolite (RO7011785) and Prodrug Metabolites (RO7018822 and RO7033805) |
0.50; 0.25; 0.50; 0.50; 0.75; 0.50 | — |
| SECONDARY Half-Life (t1/2) for RO7020531, Main Active Metabolite (RO7011785) and Prodrug Metabolites (RO7018822 and RO7033805) |
2.92; 3.38; 3.96; 4.24; 3.38; 4.39 | — |
| SECONDARY Total Amount Excreted as RO7020531, RO7011785, RO7018822 and RO7033805 |
0.00; 0.00; 0.00; 22.2; 58.3; 87.0 | — |
| SECONDARY Fraction Excreted as RO7020531, RO7011785, RO7018822 and RO7033805 |
0.00; 0.00; 0.00; 59.9; 62.9; 67.1 | — |
| SECONDARY Renal Clearance of RO7020531, RO7011785, RO7018822 and RO7033805 |
536; 590; 600; 659; 115.31; 116.30 | — |
| SECONDARY Mean Concentrations of Protein and Metabolite Markers of Humoral Response |
0.1232; 0.0433; 0.0707; 0.1316; 0.1156; 0.0455 | — |
| SECONDARY Mean Fold Changes of Protein and Metabolite Markers of Humoral Response |
1.1108; 0.9522; 0.9987; 1.5327; 1.6229; 0.8087 | — |
| SECONDARY Mean Fold Changes of Markers of Transcriptional Responses |
1.0538; 1.0907; 1.9190; 4.0828; 4.3223; 0.6938 | — |
Eligibility Criteria
Inclusion Criteria
- Chinese healthy male and female participants. Healthy status is defined by absence of evidence of any active or chronic disease following a detailed medical and surgical history, a complete physical examination including vital signs, 12-lead ECG, hematology, blood chemistry, and urinalysis.
- A Body Mass Index (BMI) of 19 to less than 28 kg/m2 and a body weight of at least 45 kg.
- Negative anti-nuclear antibody (ANA) test; or positive with dilutions not greater than 1:40 and with no associated history or symptoms of potential connective tissue disease or other immune-mediated diseases.
- Women of childbearing potential: agreement to remain abstinent (refrain from heterosexual intercourse) or use contraceptive methods.
- Men: agreement to remain abstinent (refrain from heterosexual intercourse) or use contraceptive measures and refrain from donating sperm.
- Negative pregnancy test on Day -1 for female participants.
- Non-smokers, or use of < 10 cigarettes (or equivalent nicotine-containing product) per day.
Exclusion Criteria
- Pregnant (positive pregnancy test) or lactating women, and male partners of women who are pregnant or lactating.
- History of immunologically mediated disease (e.g., inflammatory bowel disease, idiopathic thrombocytopenic purpura, lupus erythematosus, autoimmune hemolytic anemia, scleroderma, severe psoriasis, rheumatoid arthritis, multiple sclerosis, or any other autoimmune disease).
- History or symptoms of any clinically significant disease including (but not limited to), neurological, cardiovascular, endocrine, respiratory, hepatic, ocular, or renal disorder (as per Investigator's judgment).
- Personal or family history of congenital long QT syndrome or sudden cardiac death.
- Evidence of an active or suspected cancer or a history of malignancy, where in the Investigator's opinion, there is a risk of recurrence.
- History of having received or currently receiving any systemic anti-neoplastic (including radiation) or immune-modulatory treatment (including systemic oral or inhaled corticosteroids, IFN or PEG-IFN) within 6 months prior to the first dose of study drug or the expectation that such treatment will be needed at any time during the study. Eye drop-containing and infrequent inhaled corticosteroids are permissible up to 4 weeks prior to the first dose of study drug.
- History of clinically significant thyroid disease; also, subjects with clinically significant elevated thyroid-stimulating hormone (TSH) concentrations at Screening.
- Any confirmed clinically significant allergic reactions (anaphylaxis) against any drug, or multiple drug allergies (non-active hay fever is acceptable).
- Abnormal renal function.
- Alanine aminotransferase (ALT) or aspartate aminotransferase (AST) values at Screening above ULN and judged clinically significant by the Investigator.
- Positive results for anti-mitochondrial antibody (AMA), anti-smooth muscle antibody (ASMA) or thyroid peroxidase antibody.
- Positive hepatitis A IgM antibody (HAV Ab IgM), hepatitis B surface antigen (HBsAg), hepatitis C antibody (HCV Ab), or positive for human immunodeficiency virus (HIV) at Screening.
Data sourced from ClinicalTrials.gov (NCT03530917). Outcome figures and adverse-event rates are extracted automatically from the registry's posted results and are provided for clinician reference, not as a substitute for the primary publication. Informational only — not medical advice.