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Sitagliptin

Phase 1

Type II Diabetes | Small molecule | Metabolic |Novartis AG|Last Updated: Dec 17, 2020

Success Probability
Approval Probability 71%
TA Base Rate26%
Adjusted LOA41%
ML RiskLOW_RISK
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Market & Valuation
rNPV $3.2B
Market Size $9.4B
Revenue Basis $1.6B
Competitors 6
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Trial Design
Double-BlindPLACEBO_CONTROLLEDBiomarker
Total Trials1
Total Enrollment220
FDA Designations
No designations recorded
Clinical Trials (1)
NCT IDTitlePhaseStatusEnrollmentVelocityDesignStartCompletionLast UpdatedSitesCountries
NCT01619332Clinical Safety, Tolerability, Pharmacokinetics and Pharmacodynamics of LEZ763PHASE1 COMPLETED 220 — — Mar 1, 2012Sep 1, 2013Dec 17, 20206 United States
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Study Endpoints
Primary Endpoints
Number of Patients with adverse events, serious adverse events and death
Day 28

An adverse event is the appearance or worsening of any undesirable sign, symptom, or medical condition occurring after starting the study drug even if the event is not considered to be related to study drug. Adverse events will also be determined on the basis of clinical laboratory assessments, electrocardiographic evaluations and vital signs determinations.

Pharmacokinetics of LEZ763 (Part I): area under the plasma concentration-time curve from time zero to infinity (AUCinf)
pre-dose, and 0.5, 0.66, 0.75, 1, 1.5, 2, 2.5, 3, 3.5 4, 6, 8, 12 hours post-dose on Day 1; 24 and 36 hours Day 2; Day 3, Day 4

Blood will be collected at multiple timepoints and will be analyzed for LEZ736 concentrations after single dose

Pharmacokinetics of LEZ763 (Part I): area under the plasma concentration-time curve from time zero to the time of the last quantifiable concentration (AUClast)
pre-dose, and 0.5, 0.66, 0.75, 1, 1.5, 2, 2.5, 3, 3.5 4, 6, 8, 12 hours post-dose on Day 1; 24 and 36 hours Day 2; Day 3, Day 4

Blood will be collected at multiple timepoints and will be analyzed for LEZ736 concentrations after single dose

Pharmacokinetics of LEZ763 (Part I): Terminal elimination half-life (T1/2)
pre-dose, and 0.5, 0.66, 0.75, 1, 1.5, 2, 2.5, 3, 3.5 4, 6, 8, 12 hours post-dose on Day 1; 24 and 36 hours Day 2; Day 3, Day 4

Blood will be collected at multiple timepoints and will be analyzed for LEZ736 concentrations after single dose

Pharmacokinetics of LEZ763 (Part I): Apparent systemic (or total body) clearance from plasma following extravascular administration (CL/F)
pre-dose, and 0.5, 0.66, 0.75, 1, 1.5, 2, 2.5, 3, 3.5 4, 6, 8, 12 hours post-dose on Day 1; 24 and 36 hours Day 2; Day 3, Day 4

Blood will be collected at multiple timepoints and will be analyzed for LEZ736 concentrations after single dose

Pharmacokinetics of LEZ763 (Part I) : Observed maximum plasma concentration (Cmax) following drug administration
pre-dose, and 0.5, 0.66, 0.75, 1, 1.5, 2, 2.5, 3, 3.5 4, 6, 8, 12 hours post-dose on Day 1; 24 and 36 hours Day 2; Day 3, Day 4

Blood will be collected at multiple timepoints and will be analyzed for LEZ736 concentrations after single and multiple doses

Pharmacokinetics of LEZ763 (Part I): time to reach the maximum concentration after drug administration (Tmax)
pre-dose, and 0.5, 0.66, 0.75, 1, 1.5, 2, 2.5, 3, 3.5 4, 6, 8, 12 hours post-dose on Day 1; 24 and 36 hours Day 2; Day 3, Day 4

Blood will be collected at multiple timepoints and will be analyzed for LEZ736 concentrations after single dose

Pharmacokinetics of LEZ763 (Part II) : Observed maximum plasma concentration (Cmax) following drug administration
pre-dose, and 0.5, 0.66, 0.75, 1, 1.5, 2, 2.5, 3, 3.5 4, 6, 8, 12 hours post-dose on Day 1 and Day 10

Blood will be collected at multiple timepoints and will be analyzed for LEZ736 concentrations after multiple doses

Pharmacokinetics of LEZ763 (Part II): time to reach the maximum concentration after drug administration (Tmax)
pre-dose, and 0.5, 0.66, 0.75, 1, 1.5, 2, 2.5, 3, 3.5 4, 6, 8, 12 hours post-dose on Day 1 and Day 10

Blood will be collected at multiple timepoints and will be analyzed for LEZ736 concentrations after multiple doses

Pharmacokinetics of LEZ763 (Part II): Accumulation ratio(Racc)
pre-dose, and 0.5, 0.66, 0.75, 1, 1.5, 2, 2.5, 3, 3.5 4, 6, 8, 12 hours post-dose on Day 1 and Day 27

Blood will be collected at multiple timepoints and will be analyzed for LEZ736 concentrations after multiple doses

Pharmacokinetics of LEZ763 (Part III) : Observed maximum plasma concentration (Cmax) following drug administration
pre-dose, and 0.5, 0.66, 0.75, 1, 1.5, 2, 2.5, 3, 3.5 4, 6, 8, 12 hours post-dose on Day 1 and Day 27

Blood will be collected at multiple timepoints and will be analyzed for LEZ736 concentrations after multiple doses

Pharmacokinetics of LEZ763 (Part III): time to reach the maximum concentration after drug administration (Tmax)
pre-dose, and 0.5, 0.66, 0.75, 1, 1.5, 2, 2.5, 3, 3.5 4, 6, 8, 12 hours post-dose on Day 1 and Day 27

Blood will be collected at multiple timepoints and will be analyzed for LEZ736 concentrations after multiple doses

Pharmacokinetics of LEZ763 (Part III): Area under the plasma concentration-time curve from time zero to the end of the dosing interval tau (AUCtau)
pre-dose, and 0.5, 0.66, 0.75, 1, 1.5, 2, 2.5, 3, 3.5 4, 6, 8, 12 hours post-dose on Day 1 and Day 27

Blood will be collected at multiple timepoints and will be analyzed for LEZ736 concentrations after single and multiple doses

Pharmacokinetics of LEZ763 (Part III): Accumulation ratio(Racc)
pre-dose, and 0.5, 0.66, 0.75, 1, 1.5, 2, 2.5, 3, 3.5 4, 6, 8, 12 hours post-dose on Day 1 and Day 27

Blood will be collected at multiple timepoints and will be analyzed for LEZ736 concentrations after single and multiple doses

Pharmacokinetics of LEZ763 and Sitagliptin (Part III): Observed maximum plasma concentration (Cmax) following drug administration
pre-dose, and 0.5, 0.66, 0.75, 1, 1.5, 2, 2.5, 3, 3.5 and 4 hours post-dose on Day 28

Blood will be collected at multiple timepoints and will be analyzed for LEZ736 concentrations after multiple doses

Pharmacokinetics of LEZ763 and Sitagliptin (Part III): Area under the plasma concentration-time curve from time zero to the end of the dosing interval tau (AUCtau)
pre-dose, and 0.5, 0.66, 0.75, 1, 1.5, 2, 2.5, 3, 3.5 and 4 hours post-dose on Day 28

Blood will be collected at multiple timepoints and will be analyzed for LEZ736 concentrations after multiple doses

Pharmacokinetics of LEZ763 and Sitagliptin (Part III): Time to reach the maximum concentration after drug administration (Tmax)
pre-dose, and 0.5, 0.66, 0.75, 1, 1.5, 2, 2.5, 3, 3.5 and 4 hours post-dose on Day 28

Blood will be collected at multiple timepoints and will be analyzed for LEZ736 concentrations after multiple doses

Area under the effect curve (AUC0-4h) over the 4-hour post-dose period to measure glucose response following a standard mixed meal test
4 hour post-dose Day 27
Secondary Endpoints
Area under the serum Glucagon-like-peptide 1 (GLP-1) curve (AUC0-24 hours)
Pre-dose, and 0.5, 0.66, 0.75, 1, 1.5, 2, 2.5, 3, 3.5 and 4 hours post-dose on Day -1, Day 1, Day 27, and Day 28
2-hour value of post-prandial glucose
Day 1 of Part I, Day 1 and day 10 of Part II
Change from baseline in Fasting C-peptide at Day 27 (Part III)
Baseline, Day 27
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Study Design & Arms
MaskingQUADRUPLE
ModelPARALLEL
PurposeTREATMENT
Treatment Arms
ArmTypeDescription
LEZ763EXPERIMENTALPart I- Healthy volunteers enrolled into 6 single-ascending dose cohorts Part II- Healthy volunteers enrolled into 5 multiple-ascending dose cohorts. Part III- LEZ763 will be given orally once daily for 28 days in a randomized and blinded manner
PlaceboPLACEBO_COMPARATORPart I : Healthy volunteers enrolled in 6 single ascending dose cohorts to receive matching placebo of LEZ763. Part II: Healthy volunteers enrolled in 5 multiple ascending dose cohorts to receive matching placebo of LEZ763. Part III- Placebo will be given orally once daily for 28 days to patients assigned to placebo in a randomized and blinded manner
SitagliptinACTIVE_COMPARATORSitaglitpin will be given orally once daily for 28 days to patients assigned to this treatment in a randomized and blinded manner
Interventions
NameTypeDescription
PlaceboDRUGPlacebo will be given orally once daily for 28 days to patients assigned to placebo in a randomized and blinded manner
SitagliptinDRUGSitaglitpin will be given orally once daily for 28 days to patients assigned to this treatment in a randomized and blinded manner
LEZ763DRUGLEZ763 will be given orally once daily for 28 days in a randomized and blinded manner
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Eligibility Criteria
Age Range18 Years — 65 Years
SexALL
Healthy VolunteersYes
Study Sites6

Inclusion criteria: * All subjects: (suggest this will reduce duplication) * Male or female aged 18-65 yr, * Subjects must weigh at least 50 kg to participate in the study. Body mass index (BMI) must be within the range of 18-37 kg/m2 (inclusive * Only postmenopausal females or female subjects who ...

Countries:United States
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Competitive Landscape -Diabetes Complications 6 trials
CompanyTickerTrialsLead PhaseDrugs
FibroBiologics, Inc.FBLG1PHASE1Undisclosed
MiMedx Group, Inc.MDXG2NAUndisclosed
Integra LifeSciences Holdings CorporationIART1NAUndisclosed
Organogenesis Holdings, Inc. Class AORGO1NAUndisclosed
Healthcare Services Group, Inc.HCSG1NAUndisclosed
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