A Clinical Study of the HIV Drug CPT31 in Healthy Volunteers

A Phase Ia Clinical Study of HIV Entry Inhibitor CPT31: Single Ascending Dose Study of Safety, Tolerability, Immunogenicity, and Pharmacokinetics in Healthy Adults

Status

Completed

Phases

Phase 1

Study type

Interventional

Source

ClinicalTrials.gov

Registry ID

NCT04672083

Enrollment

Registered

2020-12-17

Start date

2020-11-16

Completion date

2021-04-29

Last updated

2023-02-21

For informational purposes only — not medical advice. Sourced from public registries and may not reflect the latest updates. Terms

Conditions

HIV Infections

Keywords

D-peptide HIV entry inhibitor

Brief summary

This first-in-human study will evaluate the safety, tolerability, immunogenicity, and pharmacokinetics of the HIV entry inhibitor CPT31 (cholesterol-PIE12-2-trimer) in healthy adults. This is a randomized, placebo-controlled, double-blind, single ascending dose study.

Detailed description

This is a single subcutaneous (SC) dose study. Doses will be administered in an escalating manner following satisfactory review by a Protocol Safety Review Team (PSRT) of the safety, tolerability and pharmacokinetic (PK) data through Day 6 from the lower dose levels. 32 healthy subjects will be studied in 4 groups (Groups A1 to A4). This study will comprise a placebo-controlled, double-blind, single-dose, sequential-group design in healthy subjects. Each subject will participate in 1 treatment period and reside in the Clinical Research Unit (CRU) from Day -1 through Day 6. It is planned for 6 subjects per dose level group to receive SC CPT31 and 2 subjects to receive matching placebo. Each group will be divided into 2 cohorts, with each cohort being dosed 72 hours apart. Sentinel dosing will take place in the first cohort, which will comprise 2 subjects, with 1 subject receiving CPT31 and 1 subject receiving placebo. The second cohort will comprise 6 subjects, with 5 subjects receiving CPT31 and 1 subject receiving placebo. Blood samples for PK analysis and assessment of immunogenicity will be collected predose and up to 5 days postdose, with an additional immunogenicity sample taken at the Follow-up visit.

Interventions

DRUGCPT31

CPT31 (cholesterol-PIE12-2-trimer) is a novel D-peptide HIV entry inhibitor that binds with high affinity to a conserved hydrophobic pocket within the gp41 trimer

DRUGPlacebo

matching placebo

Study design

Allocation

RANDOMIZED

Intervention model

PARALLEL

Primary purpose

TREATMENT

Masking

QUADRUPLE (Subject, Caregiver, Investigator, Outcomes Assessor)

Eligibility

Sex/Gender

ALL

Age

18 Years to 55 Years

Healthy volunteers

Yes

Inclusion criteria

* Males or females, of any race, between 18 and 55 years of age, inclusive. * Body mass index between 18.0 and 32.0 kg/m2, inclusive. * In good health, determined by no clinically significant findings from medical and surgical history, physical examination, 12 lead ECG, vital signs measurements, and clinical laboratory evaluations (congenital nonhemolytic hyperbilirubinemia \[e.g., suspicion of Gilbert's syndrome based on total and direct bilirubin\] is not acceptable) at Screening and/or Day -1 as assessed by the Investigator (or designee). * Females will not be pregnant or have been within the previous 3 months, or lactating, and females of childbearing potential and males will agree to use contraception. * Able to comprehend and willing to sign an Informed Consent Form (ICF) and to abide by the study restrictions.

Exclusion criteria

* Significant history or clinical manifestation of any metabolic, allergic, dermatological, hepatic, renal, hematological, pulmonary, cardiovascular, gastrointestinal, neurological, respiratory, endocrine, or psychiatric disorder, as determined by the Investigator (or designee). * A ≥Grade 2 laboratory abnormality at Screening or Day -1 as defined by the Division of AIDS Table for Grading the Severity of Adult and Pediatric Adverse Events, Version 2.1 dated July 2017. * Estimated glomerular filtration rate (eGFR per CKD-Epi equation) of \<90 ml/min/1.73 m2. * Known sensitivity to CPT31 or any of its components. * History of significant hypersensitivity, intolerance, or allergy to any drug compound, food, or other substance, unless approved by the Investigator (or designee). * History of alcoholism or drug/chemical abuse within 2 years prior to Day -1. * Alcohol consumption of \> 21 units per week for males and \> 14 units for females. One unit of alcohol equals 12 oz (360 mL) beer, 1½ oz (45 mL) liquor, or 5 oz (150 mL) wine. * Positive urine drug screen at Screening or positive alcohol breath test result or positive urine drug screen on Day -1. * Positive HIV test as documented by Combo Ag/Ab HIV 1/HIV-2 immunoassay. * Positive hepatitis B surface antigen, positive hepatitis B core antibody with negative hepatitis B surface antibody test result, or positive hepatitis C antibody at Screening or within 3 months before first dose of study treatment. * Participation in a clinical study involving administration of an investigational drug in the past 30 days prior to dosing. * Use or intend to use any prescription or over the counter medications/products (including HIV medications being used for pre-exposure prophylaxis) other than hormone replacement therapy, oral, implantable, transdermal, injectable, or intrauterine contraceptives or acetaminophen up to 2 grams per day for no more than 3 consecutive days within 14 days prior to dosing, unless deemed acceptable by the Investigator (or designee). * Use of tobacco or nicotine containing products within 3 months prior to Day -1, or positive cotinine at Screening or Day -1. * Receipt of blood products within 2 months prior to Day -1. * Donation of blood from 3 months prior to Screening, plasma from 2 weeks prior to Screening, or platelets from 6 weeks prior to Screening. * Poor peripheral venous access. * Have previously completed or withdrawn from this study or any other study investigating CPT31 and have previously received the investigational product. * Subjects who, in the opinion of the Investigator (or designee), should not participate in this study. * Have any clinically significant abnormal ECG results constituting a risk while taking the investigational product, as determined by the Investigator, such as any of the following, as determined by single 12-lead ECG: QT interval corrected for heart rate using Fridericia's method (QTcF) \>450 ms for males and \>470 ms for females, confirmed by calculating the mean of the original value and 2 repeats; QRS duration \>120 ms confirmed by calculating the mean of the original value and 2 repeats; PR interval \>220 ms confirmed by calculating the mean of the original value and 2 repeats; findings which would make QTc measurements difficult or QTc data uninterpretable; history of additional risk factors for torsades de pointes (e.g., heart failure, hypokalemia, family history of long QT syndrome); risks related to bradycardia, for example, second or third degree atrioventricular block or sick sinus syndrome.

Design outcomes

Primary

Measure	Time frame	Description
Adverse Events	Check-in (Day -1) through Follow-up (Day 28-30)	Number of subjects experiencing serious adverse events (SAEs)

Secondary

Measure	Time frame	Description
Tmax	Day 1 predose, 0.5 h, 1 h, 2 h, 4 h, 6 h, 8 h, 10 h, 12 h, 16 h, Day 2 (24 h), Day 3 (48 h), Day 4 (72 h), Day 5 (96 h), and Day 6 (120 h)	time of maximum observed plasma concentration (h)
T1/2	Day 1 predose, 0.5 h, 1 h, 2 h, 4 h, 6 h, 8 h, 10 h, 12 h, 16 h, Day 2 (24 h), Day 3 (48 h), Day 4 (72 h), Day 5 (96 h), and Day 6 (120 h)	apparent plasma terminal elimination half-life (h)
Area Under the Concentration Curve (AUC) 0-∞	Day 1 predose, 0.5 h, 1 h, 2 h, 4 h, 6 h, 8 h, 10 h, 12 h, 16 h, Day 2 (24 h), Day 3 (48 h), Day 4 (72 h), Day 5 (96 h), and Day 6 (120 h)	area under the concentration versus time curve (AUC) from time zero to infinity (h\*ng/mL)
AUC0-tlast	Day 1 predose, 0.5 h, 1 h, 2 h, 4 h, 6 h, 8 h, 10 h, 12 h, 16 h, Day 2 (24 h), Day 3 (48 h), Day 4 (72 h), Day 5 (96 h), and Day 6 (120 h)	area under the concentration versus time curve (AUC) from time zero to time of the last quantifiable concentration (h\*ng/mL)
Total Plasma Clearance (CL/F)	Day 1 predose, 0.5 h, 1 h, 2 h, 4 h, 6 h, 8 h, 10 h, 12 h, 16 h, Day 2 (24 h), Day 3 (48 h), Day 4 (72 h), Day 5 (96 h), and Day 6 (120 h)	apparent total plasma clearance (L/h/kg)
Cmax	Day 1 predose, 0.5 h, 1 h, 2 h, 4 h, 6 h, 8 h, 10 h, 12 h, 16 h, Day 2 (24 h), Day 3 (48 h), Day 4 (72 h), Day 5 (96 h), and Day 6 (120 h)	maximum observed plasma concentration (ng/mL)
Ae	Day 1 predose, 0.5 h, 1 h, 2 h, 4 h, 6 h, 8 h, 10 h, 12 h, 16 h, Day 2 (24 h), Day 3 (48 h), Day 4 (72 h), Day 5 (96 h), and Day 6 (120 h)	amount of drug excreted in the urine (ng/mL)
Fe	Day 1 predose, 0.5 h, 1 h, 2 h, 4 h, 6 h, 8 h, 10 h, 12 h, 16 h, Day 2 (24 h), Day 3 (48 h), Day 4 (72 h), Day 5 (96 h), and Day 6 (120 h)	percentage of dose excreted unchanged in the urine (%)
Renal Clearance (CLR)	Day 1 predose, 0.5 h, 1 h, 2 h, 4 h, 6 h, 8 h, 10 h, 12 h, 16 h, Day 2 (24 h), Day 3 (48 h), Day 4 (72 h), Day 5 (96 h), and Day 6 (120 h)	renal clearance (L/h/kg)
Immunogenicity	Pre-dose on Day 1 through Follow-up (Day 28-30)	Number of subjects with measurable levels of anti-CPT31 antibodies in serum
Vz/F	Day 1 predose, 0.5 h, 1 h, 2 h, 4 h, 6 h, 8 h, 10 h, 12 h, 16 h, Day 2 (24 h), Day 3 (48 h), Day 4 (72 h), Day 5 (96 h), and Day 6 (120 h)	apparent volume of distribution (L/kg)

Countries

United States

Participant flow

Recruitment details

Participants were recruited at a single site in the United States between 16 November 2020 (date of first informed consent) and 29 April 2021 (date of last subject's last assessment).

Pre-assignment details

32 subjects met inclusion criteria and were randomized to treatment.

Participants by arm

Arm	Count
Cohort 1 0.10 mg/kg CPT31 6 subjects receiving a single subcutaneous injection of CPT31 (0.01 mg/kg) CPT31: CPT31 (cholesterol-PIE12-2-trimer) is a novel D-peptide HIV entry inhibitor that binds with high affinity to a conserved hydrophobic pocket within the gp41 trimer	6
Cohort 2 0.04 mg/kg CPT31 6 subjects receiving a single subcutaneous injection of CPT31 (0.04 mg/kg) CPT31: CPT31 (cholesterol-PIE12-2-trimer) is a novel D-peptide HIV entry inhibitor that binds with high affinity to a conserved hydrophobic pocket within the gp41 trimer	6
Cohort 3 0.12 mg/kg CPT31 6 subjects receiving a single subcutaneous injection of CPT31 (0.12 mg/kg) CPT31: CPT31 (cholesterol-PIE12-2-trimer) is a novel D-peptide HIV entry inhibitor that binds with high affinity to a conserved hydrophobic pocket within the gp41 trimer	6
Cohort 4 0.24 mg/kg CPT31 6 subjects receiving a single subcutaneous injection of CPT31 (0.24 mg/kg) CPT31: CPT31 (cholesterol-PIE12-2-trimer) is a novel D-peptide HIV entry inhibitor that binds with high affinity to a conserved hydrophobic pocket within the gp41 trimer	6
Placebo 8 subjects receiving a single subcutaneous placebo injection	8
Total	32

Withdrawals & dropouts

Period	Reason	FG000	FG001	FG002	FG003	FG004
Overall Study	Lost to Follow-up	1	0	0	0	0

Baseline characteristics

Characteristic	Cohort 1 0.10 mg/kg CPT31	Cohort 2 0.04 mg/kg CPT31	Cohort 3 0.12 mg/kg CPT31	Cohort 4 0.24 mg/kg CPT31	Placebo	Total
Age, Categorical <=18 years	0 Participants	0 Participants	0 Participants	0 Participants	0 Participants	0 Participants
Age, Categorical >=65 years	0 Participants	0 Participants	0 Participants	0 Participants	0 Participants	0 Participants
Age, Categorical Between 18 and 65 years	6 Participants	6 Participants	6 Participants	6 Participants	8 Participants	32 Participants
Age, Continuous	41.0 years STANDARD_DEVIATION 11.26	41.8 years STANDARD_DEVIATION 9.28	25.2 years STANDARD_DEVIATION 10.25	38.7 years STANDARD_DEVIATION 11.08	38.5 years STANDARD_DEVIATION 10.77	37.1 years STANDARD_DEVIATION 11.54
Body Mass Index (BMI)	24.32 kg/m^2 STANDARD_DEVIATION 5.426	27.08 kg/m^2 STANDARD_DEVIATION 2.567	23.45 kg/m^2 STANDARD_DEVIATION 3.026	25.47 kg/m^2 STANDARD_DEVIATION 2.233	25.00 kg/m^2 STANDARD_DEVIATION 2.898	25.06 kg/m^2 STANDARD_DEVIATION 3.38
Ethnicity (NIH/OMB) Hispanic or Latino	1 Participants	3 Participants	4 Participants	3 Participants	5 Participants	16 Participants
Ethnicity (NIH/OMB) Not Hispanic or Latino	5 Participants	3 Participants	2 Participants	3 Participants	3 Participants	16 Participants
Ethnicity (NIH/OMB) Unknown or Not Reported	0 Participants	0 Participants	0 Participants	0 Participants	0 Participants	0 Participants
Race (NIH/OMB) American Indian or Alaska Native	0 Participants	0 Participants	0 Participants	0 Participants	0 Participants	0 Participants
Race (NIH/OMB) Asian	0 Participants	1 Participants	0 Participants	0 Participants	0 Participants	1 Participants
Race (NIH/OMB) Black or African American	3 Participants	4 Participants	2 Participants	1 Participants	2 Participants	12 Participants
Race (NIH/OMB) More than one race	0 Participants	0 Participants	0 Participants	0 Participants	0 Participants	0 Participants
Race (NIH/OMB) Native Hawaiian or Other Pacific Islander	0 Participants	0 Participants	0 Participants	0 Participants	0 Participants	0 Participants
Race (NIH/OMB) Unknown or Not Reported	0 Participants	0 Participants	0 Participants	0 Participants	0 Participants	0 Participants
Race (NIH/OMB) White	3 Participants	1 Participants	4 Participants	5 Participants	6 Participants	19 Participants
Region of Enrollment United States	6 participants	6 participants	6 participants	6 participants	8 participants	32 participants
Sex: Female, Male Female	3 Participants	3 Participants	2 Participants	1 Participants	2 Participants	11 Participants
Sex: Female, Male Male	3 Participants	3 Participants	4 Participants	5 Participants	6 Participants	21 Participants

Adverse events

Event type	EG000 affected / at risk	EG001 affected / at risk	EG002 affected / at risk	EG003 affected / at risk	EG004 affected / at risk
deaths Total, all-cause mortality	0 / 6	0 / 6	0 / 6	0 / 6	0 / 8
other Total, other adverse events	0 / 6	0 / 6	2 / 6	5 / 6	1 / 8
serious Total, serious adverse events	0 / 6	0 / 6	0 / 6	0 / 6	0 / 8

Outcome results

Primary

Adverse Events

Number of subjects experiencing serious adverse events (SAEs)

Time frame: Check-in (Day -1) through Follow-up (Day 28-30)

Population: The safety population included all subjects who received at least 1 dose of study treatment (CPT31 or placebo).

Arm	Measure	Value (NUMBER)
Cohort 1 0.01 mg/kg CPT31	Adverse Events	0 participants experiencing adverse events
Cohort 2 0.04 mg/kg CPT31	Adverse Events	0 participants experiencing adverse events
Cohort 3 0.12 mg/kg CPT31	Adverse Events	0 participants experiencing adverse events
Cohort 4 0.24 mg/kg CPT31	Adverse Events	0 participants experiencing adverse events
Placebo	Adverse Events	0 participants experiencing adverse events

Secondary

Ae

amount of drug excreted in the urine (ng/mL)

Time frame: Day 1 predose, 0.5 h, 1 h, 2 h, 4 h, 6 h, 8 h, 10 h, 12 h, 16 h, Day 2 (24 h), Day 3 (48 h), Day 4 (72 h), Day 5 (96 h), and Day 6 (120 h)

Population: Concentrations for all subjects in Cohorts 1-3 were below the limit of quantitation. Urine was not collected for Cohort 4.

Arm	Measure	Value (MEAN)
Cohort 1 0.01 mg/kg CPT31	Ae	NA ng/mL
Cohort 2 0.04 mg/kg CPT31	Ae	NA ng/mL
Cohort 3 0.12 mg/kg CPT31	Ae	NA ng/mL

Comparison: Concentrations for all subjects in Cohorts 1-3 were below the limit of quantification.p-value: <0.05Regression, Linear

Secondary

Area Under the Concentration Curve (AUC) 0-∞

area under the concentration versus time curve (AUC) from time zero to infinity (h\*ng/mL)

Time frame: Day 1 predose, 0.5 h, 1 h, 2 h, 4 h, 6 h, 8 h, 10 h, 12 h, 16 h, Day 2 (24 h), Day 3 (48 h), Day 4 (72 h), Day 5 (96 h), and Day 6 (120 h)

Population: Insufficient data for Cohorts 1\&2. No (AUC)0-∞ estimate possible for 3 subjects in Cohorts 1\&2, and 1 in Cohort 4 as a reliable regression could not be fitted to the data. Per SAP: terminal elimination rate constant (λz) will only be calculated when a reliable estimate is obtained using ≥3 data points, and adjusted coefficient for determination of exponential fit (R2-adj) of the regression line is ≥0.7. Parameters requiring λz will only be calculated if R2-adj value of the regression is ≥0.7.

Arm	Measure	Value (MEAN)
Cohort 1 0.01 mg/kg CPT31	Area Under the Concentration Curve (AUC) 0-∞	NA h*ng/mL
Cohort 2 0.04 mg/kg CPT31	Area Under the Concentration Curve (AUC) 0-∞	NA h*ng/mL
Cohort 3 0.12 mg/kg CPT31	Area Under the Concentration Curve (AUC) 0-∞	8170 h*ng/mL
Cohort 4 0.24 mg/kg CPT31	Area Under the Concentration Curve (AUC) 0-∞	21200 h*ng/mL

Comparison: The lack of fit test will be conducted for the statistical assessment of linearity assumption (AOL), and thus appropriateness of a power model. PK parameter is dose proportional if AOL is ruled acceptable and the 95% CI for the slope spans 1. If the AOL is ruled unacceptable for any PK parameter, its corresponding PK parameter normalized by dose administered will be ln-transformed and analyzed using an analysis of variance (ANOVA) model. The model will include dose as a factor.p-value: <0.05Regression, Linear

Secondary

AUC0-tlast

area under the concentration versus time curve (AUC) from time zero to time of the last quantifiable concentration (h\*ng/mL)

Time frame: Day 1 predose, 0.5 h, 1 h, 2 h, 4 h, 6 h, 8 h, 10 h, 12 h, 16 h, Day 2 (24 h), Day 3 (48 h), Day 4 (72 h), Day 5 (96 h), and Day 6 (120 h)

Population: The PK population included all subjects who received at least 1 dose of CPT31 and had evaluable PK data.

Arm	Measure	Value (MEAN)
Cohort 1 0.01 mg/kg CPT31	AUC0-tlast	253 h*ng/mL
Cohort 2 0.04 mg/kg CPT31	AUC0-tlast	1660 h*ng/mL
Cohort 3 0.12 mg/kg CPT31	AUC0-tlast	7000 h*ng/mL
Cohort 4 0.24 mg/kg CPT31	AUC0-tlast	19500 h*ng/mL

Secondary

Cmax

maximum observed plasma concentration (ng/mL)

Time frame: Day 1 predose, 0.5 h, 1 h, 2 h, 4 h, 6 h, 8 h, 10 h, 12 h, 16 h, Day 2 (24 h), Day 3 (48 h), Day 4 (72 h), Day 5 (96 h), and Day 6 (120 h)

Population: The pharmacokinetic (PK) population included all subjects who received at least 1 dose of CPT31 and had evaluable PK data.

Arm	Measure	Value (MEAN)
Cohort 1 0.01 mg/kg CPT31	Cmax	27.6 ng/mL
Cohort 2 0.04 mg/kg CPT31	Cmax	91.0 ng/mL
Cohort 3 0.12 mg/kg CPT31	Cmax	247 ng/mL
Cohort 4 0.24 mg/kg CPT31	Cmax	666 ng/mL

Comparison: CPT31 dose proportionality will be examined across dose groups using a power model approach or ANOVA model, as appropriate.PK parameters will be analyzed using a power model that will have the following form: parameter = intercept × dose\^slope + random error.~Using the natural log (ln) transformation, a power model can be expressed as a linear regression equation: ln(parameter) = intercept + slope × ln(dose) + random error. For dose proportionality, the slope = 1; for dose independence, = 0.p-value: <0.05ANOVA

Secondary

Fe

percentage of dose excreted unchanged in the urine (%)

Time frame: Day 1 predose, 0.5 h, 1 h, 2 h, 4 h, 6 h, 8 h, 10 h, 12 h, 16 h, Day 2 (24 h), Day 3 (48 h), Day 4 (72 h), Day 5 (96 h), and Day 6 (120 h)

Population: Concentrations for all subjects in Cohorts 1-3 were below the limit of quantitation. Urine was not collected for Cohort 4.

Arm	Measure	Value (MEAN)
Cohort 1 0.01 mg/kg CPT31	Fe	NA percentage of drug excreted unchanged
Cohort 2 0.04 mg/kg CPT31	Fe	NA percentage of drug excreted unchanged
Cohort 3 0.12 mg/kg CPT31	Fe	NA percentage of drug excreted unchanged

Comparison: Concentrations for all subjects in Cohorts 1-3 were below the limit of quantitationp-value: <0.05Regression, Linear

Secondary

Immunogenicity

Number of subjects with measurable levels of anti-CPT31 antibodies in serum

Time frame: Pre-dose on Day 1 through Follow-up (Day 28-30)

Arm	Measure	Value (COUNT_OF_PARTICIPANTS)
Cohort 1 0.01 mg/kg CPT31	Immunogenicity	0 Participants
Cohort 2 0.04 mg/kg CPT31	Immunogenicity	0 Participants
Cohort 3 0.12 mg/kg CPT31	Immunogenicity	1 Participants
Cohort 4 0.24 mg/kg CPT31	Immunogenicity	0 Participants
Placebo	Immunogenicity	0 Participants

Secondary

Renal Clearance (CLR)

renal clearance (L/h/kg)

Time frame: Day 1 predose, 0.5 h, 1 h, 2 h, 4 h, 6 h, 8 h, 10 h, 12 h, 16 h, Day 2 (24 h), Day 3 (48 h), Day 4 (72 h), Day 5 (96 h), and Day 6 (120 h)

Population: Concentrations for all subjects in Cohorts 1-3 were below the limit of quantitation. Urine was not collected for Cohort 4.

Arm	Measure	Value (MEAN)
Cohort 1 0.01 mg/kg CPT31	Renal Clearance (CLR)	NA L/h/kg
Cohort 2 0.04 mg/kg CPT31	Renal Clearance (CLR)	NA L/h/kg
Cohort 3 0.12 mg/kg CPT31	Renal Clearance (CLR)	NA L/h/kg

Comparison: Concentrations for all subjects in Cohorts 1-3 were below the limit of quantitationp-value: <0.05Regression, Linear

Secondary

T1/2

apparent plasma terminal elimination half-life (h)

Time frame: Day 1 predose, 0.5 h, 1 h, 2 h, 4 h, 6 h, 8 h, 10 h, 12 h, 16 h, Day 2 (24 h), Day 3 (48 h), Day 4 (72 h), Day 5 (96 h), and Day 6 (120 h)

Population: Insufficient data for Cohorts 1\&2. No t1/2 estimate possible for 3 subjects in Cohorts 1\&2, and 1 in Cohort 4 as a reliable regression could not be fitted to the data. Per SAP: terminal elimination rate constant (λz) will only be calculated when a reliable estimate is obtained using ≥3 data points, and adjusted coefficient for determination of exponential fit (R2-adj) of the regression line is ≥0.7. Parameters requiring λz will only be calculated if R2-adj value of the regression is ≥0.7.

Arm	Measure	Value (MEAN)
Cohort 1 0.01 mg/kg CPT31	T1/2	NA Hours post administration
Cohort 2 0.04 mg/kg CPT31	T1/2	NA Hours post administration
Cohort 3 0.12 mg/kg CPT31	T1/2	17.2 Hours post administration
Cohort 4 0.24 mg/kg CPT31	T1/2	15.2 Hours post administration

Comparison: The lack of fit test will be conducted for the statistical assessment of linearity assumption (AOL), and thus appropriateness of a power model. PK parameter is dose proportional if AOL is ruled acceptable and the 95% confidence interval for the slope spans 1. If the AOL is ruled unacceptable for any PK parameter, its corresponding PK parameter normalized by dose administered will be ln-transformed and analyzed using an analysis of variance (ANOVA) model. The model will include dose as a factor.p-value: <0.05Regression, Linear

Secondary

Tmax

time of maximum observed plasma concentration (h)

Time frame: Day 1 predose, 0.5 h, 1 h, 2 h, 4 h, 6 h, 8 h, 10 h, 12 h, 16 h, Day 2 (24 h), Day 3 (48 h), Day 4 (72 h), Day 5 (96 h), and Day 6 (120 h)

Population: The PK population included all subjects who received at least 1 dose of CPT31 and had evaluable PK data.

Arm	Measure	Value (MEDIAN)
Cohort 1 0.01 mg/kg CPT31	Tmax	6.00 Hours post administration
Cohort 2 0.04 mg/kg CPT31	Tmax	7.00 Hours post administration
Cohort 3 0.12 mg/kg CPT31	Tmax	7.00 Hours post administration
Cohort 4 0.24 mg/kg CPT31	Tmax	4.00 Hours post administration

Secondary

Total Plasma Clearance (CL/F)

apparent total plasma clearance (L/h/kg)

Time frame: Day 1 predose, 0.5 h, 1 h, 2 h, 4 h, 6 h, 8 h, 10 h, 12 h, 16 h, Day 2 (24 h), Day 3 (48 h), Day 4 (72 h), Day 5 (96 h), and Day 6 (120 h)

Population: Insufficient data for Cohorts 1\&2. No CL/F estimate possible for 3 subjects in Cohorts 1\&2, and 1 in Cohort 4 as a reliable regression could not be fitted to the data. Per SAP: terminal elimination rate constant (λz) will only be calculated when a reliable estimate is obtained using ≥3 data points, and adjusted coefficient for determination of exponential fit (R2-adj) of the regression line is ≥0.7. Parameters requiring λz will only be calculated if R2-adj value of the regression is ≥0.7

Arm	Measure	Value (MEAN)
Cohort 1 0.01 mg/kg CPT31	Total Plasma Clearance (CL/F)	NA L/h/kg
Cohort 2 0.04 mg/kg CPT31	Total Plasma Clearance (CL/F)	NA L/h/kg
Cohort 3 0.12 mg/kg CPT31	Total Plasma Clearance (CL/F)	17.2 L/h/kg
Cohort 4 0.24 mg/kg CPT31	Total Plasma Clearance (CL/F)	15.2 L/h/kg

Secondary

Vz/F

apparent volume of distribution (L/kg)

Time frame: Day 1 predose, 0.5 h, 1 h, 2 h, 4 h, 6 h, 8 h, 10 h, 12 h, 16 h, Day 2 (24 h), Day 3 (48 h), Day 4 (72 h), Day 5 (96 h), and Day 6 (120 h)

Population: Insufficient data for Cohorts 1\&2. No Vz/F estimate possible for 3 subjects in Cohorts 1\&2, and 1 in Cohort 4 as a reliable regression could not be fitted to the data. Per SAP: terminal elimination rate constant (λz) will only be calculated when a reliable estimate is obtained using ≥3 data points, and adjusted coefficient for determination of exponential fit (R2-adj) of the regression line is ≥0.7. Parameters requiring λz will only be calculated if R2-adj value of the regression is ≥0.7

Arm	Measure	Value (MEAN)
Cohort 1 0.01 mg/kg CPT31	Vz/F	NA L/kg
Cohort 2 0.04 mg/kg CPT31	Vz/F	NA L/kg
Cohort 3 0.12 mg/kg CPT31	Vz/F	0.365 L/kg
Cohort 4 0.24 mg/kg CPT31	Vz/F	0.248 L/kg

Source: ClinicalTrials.gov · Data processed: Feb 4, 2026

A Clinical Study of the HIV Drug CPT31 in Healthy Volunteers

Conditions

Keywords

Brief summary

Detailed description

Related papers

Interventions

Sponsors

Study design

Eligibility

Inclusion criteria

Exclusion criteria

Design outcomes

Primary

Secondary

Countries

Participant flow

Recruitment details

Pre-assignment details

Participants by arm

Withdrawals & dropouts

Baseline characteristics

Adverse events

Outcome results

Adverse Events

Ae

Area Under the Concentration Curve (AUC) 0-∞

AUC0-tlast

Cmax

Fe

Immunogenicity

Renal Clearance (CLR)

T1/2

Tmax

Total Plasma Clearance (CL/F)

Vz/F