See how many men reached the eugonadal range in the Phase 3 inTUne clinical study.
inTUne=investigational testosterone undecanoate.
The efficacy and safety of JATENZO were evaluated in 166 adult males with hypogonadism in a 4-month, open-label study1
Day of
Study
1
21
56
105
Starting Dose
JATENZO 237 mg twice daily with meals
Dose Adjustments
JATENZO dose adjusted on Days 21 and 56 (minimum 158 mg BID and maximum 396 mg BID) based on average testosterone concentration obtained over 24 hours post-morning dose
Final Analysis
Primary endpoint was the percentage of men with mean total testosterone concentration (Cavg) over 24 hours within the normal eugonadal range* on the final PK visit
*Normal eugonadal range was defined as 252-907 ng/dL for blood collected in NaF-EDTA tubes.1
Key Inclusion Criteria2
Baseline Demographics2
| JATENZO (n=166) | |
| Age, Mean Years | 51.6 |
| Race Native American or Alaska Native |
0 |
| Asian | 3 (1.8%) |
| African American or Black | 29 (17.5%) |
| Caucasian | 133 (80.1%) |
| Other | 1 (0.6%) |
| BMI (kg/m2), Mean | 31.8 |
| Serum Testosterone at Screen 1, Mean (ng/dL) | 190.2 |
| Duration of Hypogonadism, Mean Years | 5.9 |
| Type 1 or Type 2 Diabetes, % | 24.1 |
| History of Hypertension, % | 52.4 |
RAISE MORE THAN HIS EXPECTATIONS ABOUT ORAL TRT1,2
JATENZO raised T levels to the normal range in 87% of men.
Primary efficacy endpoint:
Exceeded FDA target of ≥75% of men in eugonadal range2
Patients taking JATENZO achieved T levels within normal eugonadal range.1-3
Average Testosterone
Concentration
Cavg (in serum): 489 ± 155 ng/dL
(mean ± SD)3*
Testosterone Cavg in normal eugonadal range was defined as 252-907 ng/dL for blood collected in NaF-EDTA tubes.1
Note that the testosterone concentrations were not measured in serum but the effects of different sample preparation conditions were accounted for in data analysis of the results shown here. The dose adjustment scheme for use in clinical practice is based on serum total testosterone.
With JATENZO (mean ± SD):
*In the inTUne study, testosterone concentrations were measured in plasma isolated from blood collected into NaF-EDTA tubes. NaF was used to limit ex vivo conversion of testosterone undecanoate to testosterone, which could artifactually raise measured testosterone levels. In a typical clinical setting, testosterone concentrations are measured in serum isolated from blood collected in plain tubes. To account for the lower testosterone concentrations measured in plasma vs serum, a conversion factor of 1.214 was determined and used to approximate the equivalent mean serum concentration of 489 ± 155 ng/dL from the mean NaF-EDTA plasma testosterone value of 403 ± 128 ng/dL in the inTUne study.1-4
Secondary endpoints:
The percentage of patients who received JATENZO and had Cmax ≤1500 ng/dL, between 1800 and 2500 ng/dL, and >2500 ng/dL at the final PK visit were 83%, 3%, and 3%, respectively.1
In the inTUne clinical study, 2% topical testosterone (T) solution was used as the active T reference arm. Testosterone Cavg was determined for each treatment group but topical T Cavg data are not included in the JATENZO labeling. The following analyses from the inTUne clinical study were exploratory. These data points are provided to reflect known pharmacological actions of TRT but were not used to assess efficacy.2,3
Average Free T
Levels2*
JATENZO
4.46
11.69
Topical TRT
4.44
9.18
Average SHBG
Levels2,3
JATENZO
28.61
17.05
Topical TRT
26.83
26.40
JATENZO
Topical TRT
*Free T concentrations were calculated using the Vermeulen formula based on T, SHBG, and albumin concentrations.3
Topical TRT study design2,3
In the inTUne trial, subjects who met all eligibility criteria were randomly assigned in a 3:1 ratio to JATENZO (n=166) or topical TRT (n=56) for 3 to 4 months. The starting dose for topical TRT was 60 mg once daily (QD) in the AM. Doses were adjusted on Days 21 and 56 (minimum 30 mg QD; maximum 120 mg QD) based on average T concentration obtained over 24 hours post-morning dose. Beyond the primary objective of the inTUne study, other objectives included comparing JATENZO-treated subjects with topical TRT-treated subjects in terms of Cavg DHT concentration at Visit 7.
Adverse reactions occurring in >2% of subjects in the topical TRT arm3: headache=1 (1.8); hematocrit increased=0; upper respiratory tract infection=0; hypertension=0; high-density lipoprotein decreased=0; nausea=0; rash=2 (3.6); overdose=2 (3.6).
DHT=dihydrotestosterone; SHBG=sex hormone-binding globulin.
Steady state by Day 76*
JATENZO maintained normal T levels over each12-hour dosing interval8‡
JATENZO Over 24 Hours1,4,8
*In a 28-day study, the results suggest that the initial transient effect is resolved by Days 5-7, and that if testosterone administration continues beyond that time, systemic concentrations remain essentially constant from at least Day 7 onward for the remainder of the study period.6
†In a 12-month study, the pharmacokinetics of oral TU were stable over an extended time period (>9 months) of chronic dosing. Steady state exposures for the oral TU treatment subjects did not change between Day 90 (after at least 1 month on the maintenance dose) and Day 365 (after at least 10 months on the maintenance dose).7
‡Note that the testosterone concentrations were not measured in serum but the effects of different sample preparation conditions were accounted for in data analysis of the results shown here. The dose adjustment scheme for use in clinical practice is based on serum total testosterone.1
Number (%) of patients with adverse reactions ≥2% in the 4-month inTUne study1
Adverse Reactions with JATENZO
| Headache | Overall (N=166) 8 (4.8%) |
|---|---|
| Hematocrit Increased | 8 (4.8%) |
| Hypertension | 6 (3.6%) |
| High-Density Lipoprotein Decreased | 5 (3.0%) |
| Nausea | 4 (2.4%) |
In the inTUne study, 3 of the 166 patients (1.8%) experienced adverse reactions that led to premature discontinuation from the study, including rash (n=1) and headache (n=2).
Adverse reactions reported in >2% of patients in all Phase 2 and 3 JATENZO trials combined (N=569):
Polycythemia, diarrhea, dyspepsia, eructation, peripheral edema, nausea, increased hematocrit, headache, prostatomegaly, and hypertension.
Mean Hematocrit2,9
JATENZO
44.5%
47.1%
Topical TRT
44.1%
46.1%
JATENZO
Topical TRT
In the inTUne clinical study, 2% topical testosterone (T) solution was used as the active T reference arm. Testosterone Cavg was determined for each treatment group but topical T Cavg data are not included in the JATENZO labeling. The following analyses from the inTUne clinical study were exploratory. These data are provided to reflect known pharmacological actions of TRT but were not used to assess safety.
Evaluate hematocrit approximately every 3 months while the patient is on JATENZO.1 All testosterone therapies, including JATENZO, require ongoing monitoring of hematocrit levels.1,10
TRT=testosterone replacement therapy.
Topical TRT study design2,3
In the inTUne trial, subjects who met all eligibility criteria were randomly assigned in a 3:1 ratio to JATENZO (n=166) or topical TRT (n=56) for 3 to 4 months. The starting dose for topical TRT was 60 mg once daily (QD) in the AM. Doses were adjusted on Days 21 and 56 (minimum 30 mg QD; maximum 120 mg QD) based on average T concentration obtained over 24 hours post-morning dose. Beyond the primary objective of the inTUne study, other objectives included comparing JATENZO-treated subjects with topical TRT-treated subjects in terms of Cavg DHT concentration at Visit 7.
Adverse reactions occurring in >2% of subjects in the topical TRT arm3: headache=1 (1.8); hematocrit increased=0; upper respiratory tract infection=0; hypertension=0; high-density lipoprotein decreased=0; nausea=0; rash=2 (3.6); overdose=2 (3.6).
In the inTUne clinical study, 2% topical testosterone (T) solution was used as the active T reference arm. Testosterone Cavg was determined for each treatment group but topical T Cavg data are not included in the JATENZO labeling. The following analyses from the inTUne clinical study were exploratory. These data are provided to reflect known pharmacological actions of TRT but were not used to assess safety.
Instruct patients about the importance of monitoring blood pressure periodically while on JATENZO.1
Blood Pressure
| Mean change in blood pressure: baseline to day 139 | JATENZO | Topical TRT | |
|---|---|---|---|
| Cuff (mmHg) | Systolic | 2.8 | 1.8 |
| Diastolic | 0.6 | 0.6 | |
| 24-hr average ABPM (mmHg) | Systolic | 4.9 | 0.2 |
| Diastolic | 2.6 | 0.4 |
Topical TRT study design2,3
In the inTUne trial, subjects who met all eligibility criteria were randomly assigned in a 3:1 ratio to JATENZO (n=166) or topical TRT (n=56) for 3 to 4 months. The starting dose for topical TRT was 60 mg once daily (QD) in the AM. Doses were adjusted on Days 21 and 56 (minimum 30 mg QD; maximum 120 mg QD) based on average T concentration obtained over 24 hours post-morning dose. Beyond the primary objective of the inTUne study, other objectives included comparing JATENZO-treated subjects with topical TRT-treated subjects in terms of Cavg DHT concentration at Visit 7.
Adverse reactions occurring in >2% of subjects in the topical TRT arm3: headache=1 (1.8); hematocrit increased=0; upper respiratory tract infection=0; hypertension=0; high-density lipoprotein decreased=0; nausea=0; rash=2 (3.6); overdose=2 (3.6).
Please see Important Safety Information, including BOXED WARNING on increases in blood pressure.
ABPM=ambulatory blood pressure monitoring; mmHg=millimeters of mercury; TRT=testosterone replacement therapy.
In the inTUne clinical study, 2% topical testosterone (T) solution was used as the active T reference arm. Testosterone Cavg was determined for each treatment group but topical T Cavg data are not included in the JATENZO labeling. The following analyses from the inTUne clinical study were exploratory. These data are provided to reflect known pharmacological actions of TRT but were not used to assess safety.
Liver Function Tests
ALT
JATENZO
34.95
31.41
Topical TRT
34.24
30.16
ALP
JATENZO
76.13
64.73
Topical TRT
80.80
77.08
AST
JATENZO
27.28
26.91
Topical TRT
26.89
25.15
Bilirubin
JATENZO
9.27
8.47
Topical TRT
10.24
10.55
JATENZO
Topical TRT
Topical TRT study design2,3
In the inTUne trial, subjects who met all eligibility criteria were randomly assigned in a 3:1 ratio to JATENZO (n=166) or topical TRT (n=56) for 3 to 4 months. The starting dose for topical TRT was 60 mg once daily (QD) in the AM. Doses were adjusted on Days 21 and 56 (minimum 30 mg QD; maximum 120 mg QD) based on average T concentration obtained over 24 hours post-morning dose. Beyond the primary objective of the inTUne study, other objectives included comparing JATENZO-treated subjects with topical TRT-treated subjects in terms of Cavg DHT concentration at Visit 7.
Adverse reactions occurring in >2% of subjects in the topical TRT arm3: headache=1 (1.8); hematocrit increased=0; upper respiratory tract infection=0; hypertension=0; high-density lipoprotein decreased=0; nausea=0; rash=2 (3.6); overdose=2 (3.6).
Additional Details:
Two oral TU patients experienced increases in AST or ALT that were <2x the upper limit of normal (ULN) and one oral TU patient experienced an elevation of AST (<2x ULN) that returned to normal during continued oral TU treatment.3
*Final visit was defined as either Visit 7 or date of last data collection if terminated early.2
ALP=alkaline phosphatase; ALT=alanine aminotransferase; AST=aspartate aminotransferase; TRT=testosterone replacement therapy; TU=testosterone undecanoate.