Phase 1
N=75
Pharmacokinetics And Relative Bioavailability Of Bococizumab (PF-04950615; RN316) When Administered To The Abdomen, Thigh Or Upper Arm
Hypercholesterolemia
Bottom Line
View on ClinicalTrials.gov: NCT02043301 ↗Enrolled (actual)
75
Serious AEs
1.3%
Results posted
May 2019
Primary outcome: Primary: Area Under the Plasma Concentration-Time Curve From Time 0 Extrapolated to Infinite Time (AUCinf) — 175.9; 198.9; 160.3 micrograms*day/milliliter (mcg*day/mL)
Study Design & Population
- Study type
- Interventional
- Phase
- Phase 1
- Interventions
- Bococizumab (PF-04950615; RN316) (Biological)
- Age
- Adult, Older Adult · 18+ yrs
- Sex
- All
- Sponsor
- Pfizer
- Primary completion
- Nov 2014
Outcome Measures
| Outcome | Result | p-value |
|---|---|---|
| PRIMARY Area Under the Plasma Concentration-Time Curve From Time 0 Extrapolated to Infinite Time (AUCinf) |
175.9; 198.9; 160.3 | — |
| PRIMARY Maximum Observed Plasma Concentration (Cmax) |
9.68; 11.89; 8.14 | — |
| SECONDARY Area Under the Curve From Time Zero to the Time of Last Quantifiable Concentration (AUClast) |
158.8; 192.5; 152.6 | — |
| SECONDARY Time to Reach Maximum Observed Plasma Concentration (Tmax) |
5.04; 4.25; 6.93 | — |
| SECONDARY Apparent Clearance (CL/F) |
0.8521; 0.7545; 0.9352 | — |
| SECONDARY Apparent Volume of Distribution (Vz/F) |
8.84; 7.98; 11.33 | — |
| SECONDARY Terminal Elimination Half-Life (t1/2) |
7.27; 7.40; 8.53 | — |
| SECONDARY Maximum Low-density Lipoprotein Cholesterol LDL-C Lowering Effect (Emax): Absolute Value |
72.20; 75.32; 74.40 | — |
| SECONDARY Emax: Change From Baseline |
-96.88; -97.62; -90.46 | — |
| SECONDARY Emax: Percent Change From Baseline |
-57.47; -56.98; -54.96 | — |
| SECONDARY Time to Reach Maximum LDL-C Lowering (Tmax, LDL-C) |
20.96; 20.06; 14.01 | — |
| SECONDARY Area Under the LDL-C Effect Curve (AUEC): Absolute Value |
11181.64; 11682.39; 11231.39 | — |
| SECONDARY AUEC: Change From Baseline |
-2982.16; -2701.99; -2546.68 | — |
| SECONDARY AUEC: Percent Change From Baseline |
-1715.22; -1538.85; -1550.73 | — |
| SECONDARY Number of Participants With Injection Site Reactions (ISRs) by Severity |
1; 0; 2; 1; 2; 0 | — |
| SECONDARY Number of Participants With Positive Anti-Drug Antibodies (ADA) and Neutralizing Antibodies (nAb) |
6; 6; 11; 2; 2; 0 | — |
| SECONDARY Anti-Drug Antibody (ADA) Titer |
NA; NA; NA; NA; NA; 7.64 | — |
| SECONDARY Neutralizing Antibody (nAb) Titer |
NA; NA; NA; NA; NA | — |
Summary
This study aims to characterize the single dose pharmacokinetics of PF-04950616 following subcutaneous injection to the abdomen, upper arm or the thigh.
Eligibility Criteria
Inclusion Criteria
- Male and female subjects 18 to 65 years of age.
- Body Mass Index (BMI) ≤ 33 kg/m2, and total body weight of 60 kg to 90 kg (132 lbs to 198 lbs).
- Fasting LDL-C must be > 130 mg/dL (borderline high per NCEP ATP III criteria) at two qualifying visits: initial screening (Days -28 to -14) and Day -7.
Exclusion Criteria
- Poorly controlled type 1 or type 2 diabetes mellitus (HbA1c > 9.0%).
- History of a cardiovascular or cerebrovascular event (eg, MI, stroke, TIA) or related procedure (eg, angioplasty) during the past year.
- Subjects who meet the New York Heart Association (NYHA) criteria for congestive heart failure (CHF) classes III or IV.
Data sourced from ClinicalTrials.gov (NCT02043301). 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.