Study on Efficacy, Pharmacokinetics, and Safety of Two Subcutaneous Injections of Triptorelin Embonate 6 Month Formulation in Patients With Advanced Prostate Cancer

A Multicentre, Open, Non-comparative, Phase III Study on the Efficacy, Pharmacokinetics, and Safety of Two Subcutaneous Injections of Triptorelin Embonate 22.5 mg 6-month Formulation in Patients With Advanced Prostate Cancer

Status

Completed

Phases

Phase 3

Study type

Interventional

Source

ClinicalTrials.gov

Registry ID

NCT01656161

Enrollment

120

Registered

2012-08-02

Start date

2012-07-31

Completion date

2013-08-31

Last updated

2015-09-15

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

Conditions

Prostate Cancer

Brief summary

The primary purpose of this study is to evaluate the efficacy of triptorelin embonate 22.5 mg 6-month formulation administered by the subcutaneous (under the skin) route in: * achieving castrate levels of testosterone (\< 1.735 nmol/L) on Day 29 \[i.e., 28 days after investigational medicinal product (IMP) injection\], and * in maintaining serum testosterone castrate levels from Month 2 (Day 57) to end of Month 12 (Day 337) in participants with advanced prostate cancer.

Interventions

DRUGTriptorelin embonate 22.5 mg

Study design

Allocation

Intervention model

SINGLE_GROUP

Primary purpose

TREATMENT

Masking

NONE

Eligibility

Sex/Gender

MALE

Healthy volunteers

Inclusion criteria

Summary Inclusion Criteria: * Meets protocol-specified criteria for qualification and contraception * Is willing and able to remain confined in the study unit for the entire duration of each treatment period and comply with restrictions related food, drink and medications * Voluntarily consents to participate and provides written informed consent prior to any protocol-specific procedures Summary

Exclusion criteria

* Has history or current use of over-the-counter medications, dietary supplements, or drugs (including nicotine and alcohol) outside protocol-specified parameters * Has signs, symptoms or history of any condition that, per protocol or in the opinion of the investigator, might compromise: 1) the safety or well-being of the participant or study staff; 2) the safety or well-being of the participant's offspring (such as through pregnancy or breast-feeding); 3) the analysis of results

Design outcomes

Primary

Measure	Time frame
Percentage of Participants Achieving and Maintaining Castrate Levels of Serum Testosterone (<1.735 Nmol/L)	within 337 days

Secondary

Measure	Time frame
Percentage Change From Baseline in Prostate Specific Antigen (PSA) Through Day 337	Baseline through Day 337
Number of Participants Who Presented a Real Acute-on-chronic (AOC) Phenomenon (Testosterone Levels ≥ 1.735 Nmol/L 48 Hours After the Second Injection While Previously Castrated)	Day 171
Testosterone Pharmacodynamic (PD) Metrics for First Injection: Area Under the Concentration vs Time Curve (AUC)	Days 1-169
Testosterone PD Metrics for First Injection: Maximum Concentration (Cmax)	Days 1-169
Percentage of Participants Showing ≤ 1.0 IU/L Increase in Serum Luteinising Hormone (LH) From 0 Hour to 2 Hours Post-injection on Day 1 and Day 169	on Days 1 and 169
Testosterone PD Metrics for First Injection: Time to Castration (Tcast)	Days 1-169
Triptorelin PK Metrics for Both Injections: Area Under the Concentration vs Time Curve (AUC)	Days 1-169 and Days 169-337
Triptorelin PK Metrics for Both Injections: Cmax	Days 1-169 and Days 169-337
Triptorelin PK Metrics for Both Injections: Concentration 0 Hour	Days 1-169 and Days 169-337
Testosterone PD Metrics for First Injection: Time to Peak Serum/Plasma Concentration (Tmax)	Days 1-169

Countries

South Africa

Participant flow

Recruitment details

Participants took part in the study at 10 hospital settings in South Africa, from 03 July 2012 to 30 August 2013.

Participants by arm

Arm	Count
Triptorelin Embonate 22.5 mg Participants received subcutaneous injections of triptorelin embonate 22.5 mg 6-month formulation administered on Day 1 and on Day 169.	120
Total	120

Withdrawals & dropouts

Period	Reason	FG000
Overall Study	Adverse Event	2
Overall Study	Death	3
Overall Study	Protocol Violation	1
Overall Study	Withdrawal by Subject	1

Baseline characteristics

Characteristic	Triptorelin Embonate 22.5 mg
Age, Continuous	72.23 years STANDARD_DEVIATION 7.32
Region of Enrollment South Africa	120 participants
Sex: Female, Male Female	0 Participants
Sex: Female, Male Male	120 Participants

Adverse events

Event type	EG000 affected / at risk
deaths Total, all-cause mortality	— / —
other Total, other adverse events	117 / 120
serious Total, serious adverse events	17 / 120

Outcome results

Primary

Percentage of Participants Achieving and Maintaining Castrate Levels of Serum Testosterone (<1.735 Nmol/L)

Time frame: within 337 days

Population: Intention to treat population

Arm	Measure	Group	Value (NUMBER)
Triptorelin Embonate 22.5 mg	Percentage of Participants Achieving and Maintaining Castrate Levels of Serum Testosterone (<1.735 Nmol/L)	Achieving (by Day 29)	98.33 Percentage of Participants
Triptorelin Embonate 22.5 mg	Percentage of Participants Achieving and Maintaining Castrate Levels of Serum Testosterone (<1.735 Nmol/L)	Maintaining (Day 57 to Day 337)	82.61 Percentage of Participants

Secondary

Number of Participants Who Presented a Real Acute-on-chronic (AOC) Phenomenon (Testosterone Levels ≥ 1.735 Nmol/L 48 Hours After the Second Injection While Previously Castrated)

Time frame: Day 171

Arm	Measure	Value (NUMBER)
Triptorelin Embonate 22.5 mg	Number of Participants Who Presented a Real Acute-on-chronic (AOC) Phenomenon (Testosterone Levels ≥ 1.735 Nmol/L 48 Hours After the Second Injection While Previously Castrated)	1 participants

Secondary

Percentage Change From Baseline in Prostate Specific Antigen (PSA) Through Day 337

Time frame: Baseline through Day 337

Population: ITT population with a measured value at each specified time point

Arm	Measure	Group	Value (MEAN)	Dispersion
Triptorelin Embonate 22.5 mg	Percentage Change From Baseline in Prostate Specific Antigen (PSA) Through Day 337	at Day 85 (n=119)	-83.20 percentage of change in PSA levels	Standard Deviation 38.1
Triptorelin Embonate 22.5 mg	Percentage Change From Baseline in Prostate Specific Antigen (PSA) Through Day 337	at Day 169 (n=117)	-83.48 percentage of change in PSA levels	Standard Deviation 38.29
Triptorelin Embonate 22.5 mg	Percentage Change From Baseline in Prostate Specific Antigen (PSA) Through Day 337	at Day 253 (n=114)	-85.43 percentage of change in PSA levels	Standard Deviation 33.94
Triptorelin Embonate 22.5 mg	Percentage Change From Baseline in Prostate Specific Antigen (PSA) Through Day 337	at Day 337 (n=113)	-82.89 percentage of change in PSA levels	Standard Deviation 40.74

Secondary

Percentage of Participants Showing ≤ 1.0 IU/L Increase in Serum Luteinising Hormone (LH) From 0 Hour to 2 Hours Post-injection on Day 1 and Day 169

Time frame: on Days 1 and 169

Population: Intention to treat (ITT) population with a measured value at the time analysed

Arm	Measure	Group	Value (NUMBER)
Triptorelin Embonate 22.5 mg	Percentage of Participants Showing ≤ 1.0 IU/L Increase in Serum Luteinising Hormone (LH) From 0 Hour to 2 Hours Post-injection on Day 1 and Day 169	on Day 1 (n=118)	0.85 percentage of participants
Triptorelin Embonate 22.5 mg	Percentage of Participants Showing ≤ 1.0 IU/L Increase in Serum Luteinising Hormone (LH) From 0 Hour to 2 Hours Post-injection on Day 1 and Day 169	on Day 169 (n=115)	87.83 percentage of participants

Secondary

Testosterone PD Metrics for First Injection: Maximum Concentration (Cmax)

Time frame: Days 1-169

Arm	Measure	Value (GEOMETRIC_MEAN)
Triptorelin Embonate 22.5 mg	Testosterone PD Metrics for First Injection: Maximum Concentration (Cmax)	16.52 nmol/L

Secondary

Testosterone PD Metrics for First Injection: Time to Castration (Tcast)

Time frame: Days 1-169

Arm	Measure	Value (GEOMETRIC_MEAN)
Triptorelin Embonate 22.5 mg	Testosterone PD Metrics for First Injection: Time to Castration (Tcast)	18.01 days

Secondary

Testosterone PD Metrics for First Injection: Time to Peak Serum/Plasma Concentration (Tmax)

Time frame: Days 1-169

Population: PK/PD subset of 15 participants

Arm	Measure	Value (MEDIAN)	Dispersion
Triptorelin Embonate 22.5 mg	Testosterone PD Metrics for First Injection: Time to Peak Serum/Plasma Concentration (Tmax)	48 hours	95% Confidence Interval 40.02

Secondary

Testosterone Pharmacodynamic (PD) Metrics for First Injection: Area Under the Concentration vs Time Curve (AUC)

Time frame: Days 1-169

Arm	Measure	Value (GEOMETRIC_MEAN)
Triptorelin Embonate 22.5 mg	Testosterone Pharmacodynamic (PD) Metrics for First Injection: Area Under the Concentration vs Time Curve (AUC)	224.13 day*nmol/L

Secondary

Triptorelin PK Metrics for Both Injections: Area Under the Concentration vs Time Curve (AUC)

Time frame: Days 1-169 and Days 169-337

Arm	Measure	Group	Value (GEOMETRIC_MEAN)
Triptorelin Embonate 22.5 mg	Triptorelin PK Metrics for Both Injections: Area Under the Concentration vs Time Curve (AUC)	AUC(1-169)	61.30 days * ng/mL
Triptorelin Embonate 22.5 mg	Triptorelin PK Metrics for Both Injections: Area Under the Concentration vs Time Curve (AUC)	AUC(169-337)	66.44 days * ng/mL

Secondary

Triptorelin PK Metrics for Both Injections: Cmax

Time frame: Days 1-169 and Days 169-337

Arm	Measure	Group	Value (GEOMETRIC_MEAN)
Triptorelin Embonate 22.5 mg	Triptorelin PK Metrics for Both Injections: Cmax	Days 1-169	16.77 ng/mL
Triptorelin Embonate 22.5 mg	Triptorelin PK Metrics for Both Injections: Cmax	Days 169-337	18.09 ng/mL

Secondary

Triptorelin PK Metrics for Both Injections: Concentration 0 Hour

Time frame: Days 1-169 and Days 169-337

Population: Participants in the PK/PD subset with a measured value.

Arm	Measure	Group	Value (GEOMETRIC_MEAN)
Triptorelin Embonate 22.5 mg	Triptorelin PK Metrics for Both Injections: Concentration 0 Hour	Days 1-169	0.04 ng/mL
Triptorelin Embonate 22.5 mg	Triptorelin PK Metrics for Both Injections: Concentration 0 Hour	Days 169-337	0.07 ng/mL

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

Study on Efficacy, Pharmacokinetics, and Safety of Two Subcutaneous Injections of Triptorelin Embonate 6 Month Formulation in Patients With Advanced Prostate Cancer

Conditions

Brief summary

Related papers

Interventions

Sponsors

Study design

Eligibility

Inclusion criteria

Exclusion criteria

Design outcomes

Primary

Secondary

Countries

Participant flow

Recruitment details

Participants by arm

Withdrawals & dropouts

Baseline characteristics

Adverse events

Outcome results

Percentage of Participants Achieving and Maintaining Castrate Levels of Serum Testosterone (<1.735 Nmol/L)

Number of Participants Who Presented a Real Acute-on-chronic (AOC) Phenomenon (Testosterone Levels ≥ 1.735 Nmol/L 48 Hours After the Second Injection While Previously Castrated)

Percentage Change From Baseline in Prostate Specific Antigen (PSA) Through Day 337

Percentage of Participants Showing ≤ 1.0 IU/L Increase in Serum Luteinising Hormone (LH) From 0 Hour to 2 Hours Post-injection on Day 1 and Day 169

Testosterone PD Metrics for First Injection: Maximum Concentration (Cmax)

Testosterone PD Metrics for First Injection: Time to Castration (Tcast)

Testosterone PD Metrics for First Injection: Time to Peak Serum/Plasma Concentration (Tmax)

Testosterone Pharmacodynamic (PD) Metrics for First Injection: Area Under the Concentration vs Time Curve (AUC)

Triptorelin PK Metrics for Both Injections: Area Under the Concentration vs Time Curve (AUC)

Triptorelin PK Metrics for Both Injections: Cmax

Triptorelin PK Metrics for Both Injections: Concentration 0 Hour