A Clinical Study to Evaluate the Safety of CS-1103 in Healthy Participants

A Phase 1a, Randomized, Double-Blind, Placebo-Controlled, Single Center Study to Evaluate the Safety, Tolerability, and Pharmacokinetics of CS-1103 Following Single, Ascending Intravenous Dose Administration in Healthy Participants

Status

Completed

Phases

Phase 1

Study type

Interventional

Source

ClinicalTrials.gov

Registry ID

NCT06316973

Enrollment

Registered

2024-03-19

Start date

2024-02-07

Completion date

2024-06-06

Last updated

2025-11-10

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

Conditions

Substance Use Disorders, Methamphetamine Abuse, Methamphetamine Intoxication

Brief summary

The purpose of this Phase 1a study is to evaluate safety, tolerability, and pharmacokinetics (PK) of single, ascending doses of CS-1103, administered by intravenous (IV) infusion in healthy participants.

Interventions

DRUGCS-1103

CS-1103 for infusion

DRUGSterile Saline

Sterile Saline for Injection

Study design

Allocation

RANDOMIZED

Intervention model

PARALLEL

Primary purpose

TREATMENT

Masking

QUADRUPLE (Subject, Caregiver, Investigator, Outcomes Assessor)

Intervention model description

Randomized, Double-Blind, Placebo-Controlled, Single Center Study to Evaluate the Safety, Tolerability, and Pharmacokinetics of CS-1103 Following Single, Ascending Intravenous Dose Administration in Healthy Participants

Eligibility

Sex/Gender

ALL

Age

18 Years to 55 Years

Healthy volunteers

Yes

Inclusion criteria

Major Inclusion Criteria: 1. Healthy male and/or female participants aged 18 to 55 years, inclusive. 2. A body mass index between 18.0 to 30.0 kg/m2, inclusive, and a minimum body weight of 50 kg. 3. Females must be of nonchildbearing potential. Major

Exclusion criteria

1. Estimated glomerular filtration rate \<90 mL/min/1.73 m2 2. Any clinically significant abnormalities in rhythm, conduction or morphology of the resting ECG, and any clinically important abnormalities in the 12-lead ECG 3. Current smokers, or those who have smoked or used nicotine products (including nicotine patches) within 1 month prior to dose administration. 4. History of alcohol abuse or excessive intake of alcohol

Design outcomes

Primary

Measure	Time frame	Description
Number of Participants With Treatment-Emergent Adverse Events (AEs)	3 days plus 8 days for follow-up	Treatment-emergent adverse events assessed through physical examinations, vital signs (blood pressure, pulse rate, respiratory rate, oxygen saturation, and body temperature), electrocardiograms (digital 12-lead electrocardiograms (ECGs). Any correlation between CS-1103 plasma concentrations and changes in QT intervals will be noted), and laboratory parameters (clinical chemistry, hematology, coagulation, and urinalysis).
Number of Participants by Severity of AEs	3 days plus 8 days for follow-up	Severity of AEs was classified as mild, moderate, or severe (increasing severity). A subject experiencing multiple occurrences of an adverse event in a particular category was counted, at most, once for that category for each treatment.

Secondary

Measure	Time frame	Description
Plasma PK Parameter: t1/2	End-of-Infusion (EOI), 5, 10, 20, 30, 40 min, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 24, 36, 48 hr	Terminal Elimination Half-life of CS-1103
Plasma PK Parameter: CL	End-of-Infusion (EOI), 5, 10, 20, 30, 40 min, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 24, 36, 48 hr	Systemic Clearance of CS-1103
Plasma Pharmacokinetic (PK) Parameter: Cmax	End-of-Infusion (EOI), 5, 10, 20, 30, 40 min, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 24, 36, 48 hr	Maximum concentration, obtained directly from the observed concentration versus time data.
Urine PK Parameter: Fe (0-last)	Time intervals from 0-24 hours after IV administration of CS-1103	Cumulative fraction of dose excreted in urine during the pooled collection intervals. Due to inherent error in measuring CS-1103 recovered in urine, the calculated recovery may exceed 100% of the dose.
Plasma PK Parameter: Vz	End-of-Infusion (EOI), 5, 10, 20, 30, 40 min, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 24, 36, 48 hr	Volume of Distribution of CS-1103
Plasma PK Parameter: Tmax	End-of-Infusion (EOI), 5, 10, 20, 30, 40 min, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 24, 36, 48 hr	Time of maximum observed blood plasma concentration (Cmax) of CS-1103

Countries

United States

Participant flow

Participants by arm

Arm	Count
Cohort 1 (2.5 mg/kg CS-1103 [Free Acid]) 6 participants received a single dose of 2.7 mg/kg (2.5 mg/kg free acid) CS-1103 administered as solution for infusion by IV over 10 minutes. A diluted CS-1103 saline solution in an IV bag is used for drug administration.	6
Cohort 2 (7.5 mg/kg CS-1103 [Free Acid]) 6 participants received single dose of 8.0 mg/kg (7.5 mg/kg free acid) CS-1103 administered as solution for infusion by IV over 10 minutes. A diluted CS-1103 saline solution in an IV bag is used for drug administration.	6
Cohort 3 (15.1 mg/kg CS-1103 [Free Acid]) 6 participants received a single dose of 16.0 mg/kg (15.1 mg/kg free acid) CS-1103 administered as solution for infusion by IV over 10 minutes. A diluted CS-1103 saline solution in an IV bag is used for drug administration.	6
Cohort 4 (17.9 mg/kg CS-1103 [Free Acid]) 6 participants received a single dose of 19.0 mg/kg (17.9 mg/kg free acid) CS-1103 administered as solution for infusion by IV over 10 minutes. A diluted CS-1103 saline solution in an IV bag is used for drug administration.	6
Placebo 2 participants for each cohort were administered with placebo. Total administered volume of saline matched administered volume for the corresponding CS-1103 solution in each cohort.	8
Total	32

Baseline characteristics

Characteristic	Cohort 1 (2.5 mg/kg CS-1103 [Free Acid])	Total	Placebo	Cohort 4 (17.9 mg/kg CS-1103 [Free Acid])	Cohort 3 (15.1 mg/kg CS-1103 [Free Acid])	Cohort 2 (7.5 mg/kg CS-1103 [Free Acid])
Age, Continuous	29.7 years STANDARD_DEVIATION 10.7	34.9 years STANDARD_DEVIATION 9.7	36.3 years STANDARD_DEVIATION 10.4	38.5 years STANDARD_DEVIATION 7.9	39.5 years STANDARD_DEVIATION 9	30.3 years STANDARD_DEVIATION 8.3
BMI	25.815 kg/m^2 STANDARD_DEVIATION 2.479	25.487 kg/m^2 STANDARD_DEVIATION 2.624	26.161 kg/m^2 STANDARD_DEVIATION 2.308	25.975 kg/m^2 STANDARD_DEVIATION 2.602	24.528 kg/m^2 STANDARD_DEVIATION 2.731	24.728 kg/m^2 STANDARD_DEVIATION 3.451
Ethnicity (NIH/OMB) Hispanic or Latino	0 Participants	4 Participants	0 Participants	2 Participants	0 Participants	2 Participants
Ethnicity (NIH/OMB) Not Hispanic or Latino	6 Participants	28 Participants	8 Participants	4 Participants	6 Participants	4 Participants
Ethnicity (NIH/OMB) Unknown or Not Reported	0 Participants	0 Participants	0 Participants	0 Participants	0 Participants	0 Participants
Height	179.23 cm STANDARD_DEVIATION 6.59	172.68 cm STANDARD_DEVIATION 7.73	174.63 cm STANDARD_DEVIATION 5.42	171.12 cm STANDARD_DEVIATION 5.98	166.97 cm STANDARD_DEVIATION 6.65	170.80 cm STANDARD_DEVIATION 10.11
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	0 Participants	0 Participants	0 Participants	0 Participants	0 Participants
Race (NIH/OMB) Black or African American	1 Participants	18 Participants	6 Participants	2 Participants	5 Participants	4 Participants
Race (NIH/OMB) More than one race	1 Participants	1 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	4 Participants	13 Participants	2 Participants	4 Participants	1 Participants	2 Participants
Sex: Female, Male Female	0 Participants	4 Participants	0 Participants	0 Participants	3 Participants	1 Participants
Sex: Female, Male Male	6 Participants	28 Participants	8 Participants	6 Participants	3 Participants	5 Participants
Weight	83.30 kg STANDARD_DEVIATION 11.81	76.26 kg STANDARD_DEVIATION 9.6	79.44 kg STANDARD_DEVIATION 6.77	76.20 kg STANDARD_DEVIATION 9.27	68.32 kg STANDARD_DEVIATION 6.93	72.97 kg STANDARD_DEVIATION 8.3

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	1 / 6	1 / 6	2 / 6	4 / 6	0 / 8
serious Total, serious adverse events	0 / 6	0 / 6	0 / 6	0 / 6	0 / 8

Outcome results

Primary

Number of Participants by Severity of AEs

Severity of AEs was classified as mild, moderate, or severe (increasing severity). A subject experiencing multiple occurrences of an adverse event in a particular category was counted, at most, once for that category for each treatment.

Time frame: 3 days plus 8 days for follow-up

Arm	Measure	Group	Value (COUNT_OF_PARTICIPANTS)
Cohort 1 (2.5 mg/kg CS-1103 [Free Acid])	Number of Participants by Severity of AEs	Mild	1 Participants
Cohort 1 (2.5 mg/kg CS-1103 [Free Acid])	Number of Participants by Severity of AEs	Severe	0 Participants
Cohort 1 (2.5 mg/kg CS-1103 [Free Acid])	Number of Participants by Severity of AEs	Moderate	0 Participants
Cohort 2 (7.5 mg/kg CS-1103 [Free Acid])	Number of Participants by Severity of AEs	Moderate	0 Participants
Cohort 2 (7.5 mg/kg CS-1103 [Free Acid])	Number of Participants by Severity of AEs	Mild	1 Participants
Cohort 2 (7.5 mg/kg CS-1103 [Free Acid])	Number of Participants by Severity of AEs	Severe	0 Participants
Cohort 3 (15.1 mg/kg CS-1103 [Free Acid])	Number of Participants by Severity of AEs	Moderate	0 Participants
Cohort 3 (15.1 mg/kg CS-1103 [Free Acid])	Number of Participants by Severity of AEs	Mild	2 Participants
Cohort 3 (15.1 mg/kg CS-1103 [Free Acid])	Number of Participants by Severity of AEs	Severe	0 Participants
Cohort 4 (17.9 mg/kg CS-1103 [Free Acid])	Number of Participants by Severity of AEs	Mild	4 Participants
Cohort 4 (17.9 mg/kg CS-1103 [Free Acid])	Number of Participants by Severity of AEs	Severe	0 Participants
Cohort 4 (17.9 mg/kg CS-1103 [Free Acid])	Number of Participants by Severity of AEs	Moderate	0 Participants
Placebo	Number of Participants by Severity of AEs	Moderate	0 Participants
Placebo	Number of Participants by Severity of AEs	Mild	0 Participants
Placebo	Number of Participants by Severity of AEs	Severe	0 Participants

Primary

Number of Participants With Treatment-Emergent Adverse Events (AEs)

Treatment-emergent adverse events assessed through physical examinations, vital signs (blood pressure, pulse rate, respiratory rate, oxygen saturation, and body temperature), electrocardiograms (digital 12-lead electrocardiograms (ECGs). Any correlation between CS-1103 plasma concentrations and changes in QT intervals will be noted), and laboratory parameters (clinical chemistry, hematology, coagulation, and urinalysis).

Time frame: 3 days plus 8 days for follow-up

Arm	Measure	Group	Value (COUNT_OF_PARTICIPANTS)
Cohort 1 (2.5 mg/kg CS-1103 [Free Acid])	Number of Participants With Treatment-Emergent Adverse Events (AEs)	TEAEs leading to study discontinuation	0 Participants
Cohort 1 (2.5 mg/kg CS-1103 [Free Acid])	Number of Participants With Treatment-Emergent Adverse Events (AEs)	TEAEs	1 Participants
Cohort 1 (2.5 mg/kg CS-1103 [Free Acid])	Number of Participants With Treatment-Emergent Adverse Events (AEs)	TEAEs leading to death	0 Participants
Cohort 1 (2.5 mg/kg CS-1103 [Free Acid])	Number of Participants With Treatment-Emergent Adverse Events (AEs)	Related TEAEs	0 Participants
Cohort 1 (2.5 mg/kg CS-1103 [Free Acid])	Number of Participants With Treatment-Emergent Adverse Events (AEs)	Serious TEAEs	0 Participants
Cohort 2 (7.5 mg/kg CS-1103 [Free Acid])	Number of Participants With Treatment-Emergent Adverse Events (AEs)	TEAEs leading to study discontinuation	0 Participants
Cohort 2 (7.5 mg/kg CS-1103 [Free Acid])	Number of Participants With Treatment-Emergent Adverse Events (AEs)	Serious TEAEs	0 Participants
Cohort 2 (7.5 mg/kg CS-1103 [Free Acid])	Number of Participants With Treatment-Emergent Adverse Events (AEs)	Related TEAEs	0 Participants
Cohort 2 (7.5 mg/kg CS-1103 [Free Acid])	Number of Participants With Treatment-Emergent Adverse Events (AEs)	TEAEs leading to death	0 Participants
Cohort 2 (7.5 mg/kg CS-1103 [Free Acid])	Number of Participants With Treatment-Emergent Adverse Events (AEs)	TEAEs	1 Participants
Cohort 3 (15.1 mg/kg CS-1103 [Free Acid])	Number of Participants With Treatment-Emergent Adverse Events (AEs)	Serious TEAEs	0 Participants
Cohort 3 (15.1 mg/kg CS-1103 [Free Acid])	Number of Participants With Treatment-Emergent Adverse Events (AEs)	TEAEs	2 Participants
Cohort 3 (15.1 mg/kg CS-1103 [Free Acid])	Number of Participants With Treatment-Emergent Adverse Events (AEs)	Related TEAEs	1 Participants
Cohort 3 (15.1 mg/kg CS-1103 [Free Acid])	Number of Participants With Treatment-Emergent Adverse Events (AEs)	TEAEs leading to study discontinuation	0 Participants
Cohort 3 (15.1 mg/kg CS-1103 [Free Acid])	Number of Participants With Treatment-Emergent Adverse Events (AEs)	TEAEs leading to death	0 Participants
Cohort 4 (17.9 mg/kg CS-1103 [Free Acid])	Number of Participants With Treatment-Emergent Adverse Events (AEs)	TEAEs leading to death	0 Participants
Cohort 4 (17.9 mg/kg CS-1103 [Free Acid])	Number of Participants With Treatment-Emergent Adverse Events (AEs)	TEAEs	4 Participants
Cohort 4 (17.9 mg/kg CS-1103 [Free Acid])	Number of Participants With Treatment-Emergent Adverse Events (AEs)	TEAEs leading to study discontinuation	0 Participants
Cohort 4 (17.9 mg/kg CS-1103 [Free Acid])	Number of Participants With Treatment-Emergent Adverse Events (AEs)	Serious TEAEs	0 Participants
Cohort 4 (17.9 mg/kg CS-1103 [Free Acid])	Number of Participants With Treatment-Emergent Adverse Events (AEs)	Related TEAEs	4 Participants
Placebo	Number of Participants With Treatment-Emergent Adverse Events (AEs)	Serious TEAEs	0 Participants
Placebo	Number of Participants With Treatment-Emergent Adverse Events (AEs)	TEAEs leading to study discontinuation	0 Participants
Placebo	Number of Participants With Treatment-Emergent Adverse Events (AEs)	TEAEs	0 Participants
Placebo	Number of Participants With Treatment-Emergent Adverse Events (AEs)	TEAEs leading to death	0 Participants
Placebo	Number of Participants With Treatment-Emergent Adverse Events (AEs)	Related TEAEs	0 Participants

Secondary