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Corporate OverviewNovember 2016
NON-CONFIDENTIAL
Enteris BioPharmaOverview
2
Internal Pipeline • Lead product candidate, Ovarest™ (oral leuprolide tablet), to be evaluated in a Phase 2 clinical trial for its potential to treat endometriosis
• Tobrate™ (oral tobramycin tablet) is being evaluated in a Phase 1 clinical trial for its potential to treat uUTI
Clinical / Commercial Tablet Manufacturing
• Experienced clinical trial manufacturer to support our partners’ research and development needs.
• Supply of GMP clinical trial / commercial material, analytical development, and stability testing
Peptelligence™ PlatformProprietary, Cutting-Edge Oral Drug Delivery Technology
• Novel formulation technology enables oral delivery of molecules that are typically injected, including peptides and BCS class II, III, and IV small molecules
• Robust IP protection in the U.S. and abroad through 2030
Feasibility-to-Licensing Partnering Program
• Advanced oral formulation solution• Recent successes:
• Tarsa Therapeutics – NDA submitted for TBRIA™ in osteoporosis• Cara Therapeutics – Phase 2b initiated in 9/2016 in chronic pain
(osteoarthritis) and Phase 1 initiated 10/2016 in uremic pruritus
Enteris BioPharmaLeadership Team
3
Leadership History • Joel TuneExecutive Chairman & Chief Executive Officer 35+ years of pharma, medtech and biotech experience Extensive management experience in product development,
sales and marketing, strategy, M&A and general management Successfully completed more than 20 business development
transactions for Baxter Healthcare’s Medication DeliveryGroup
• Brian ZietsmanPresident & Chief Financial Officer 25+ years of strategic finance and accounting experience Diverse financial capacities with public and private
pharma/biotech companies
• Paul Shields, Ph.D.Chief Operating Officer 24+ years in the biopharma industry Extensive Chemistry, Manufacturing, and Controls (CMC)
experience
Overview of Peptelligence™Intelligent Solutions for Oral Drug Delivery™
4
• Reduces peptide degradation
• Increases paracellular transport
• No modification of the peptide required
• Permeation enhancer acts as a surfactant
• Paracellular transport bypasses transcellular permeation hurdles
5
Peptelligence™ The Peptelligence™ Solution
Oral Peptide Delivery Challenges• GI tract degrades and digests
peptides• Low permeability through the
intestinal cell layer
Oral Small Molecule Delivery Challenges• Solubility or dissolution with
limited absorption• Poor permeability due to
interaction with efflux transporters or other mechanisms
Peptelligence™ Solution
Peptelligence™ Mechanism for Oral Drug Delivery
6
Increases product uptake & use vs. parenteral administration
• Increases physician starts• Improves patient compliance• Expands indications
Protects & extends product exclusivity & commercial life
• Provides compelling differentiation in competitive markets
• Adds extra layer of robust IP protection through 2030
Mechanism for Oral Drug Delivery
Enteric coat prevents tablet from opening in stomach at low pH
API absorbed across intestinal wall via paracellular transport
Enteric coat dissolves at neutral pH in the small intestine
Protease inhibitor, permeability enhancers and API released
Peptelligence™ Bioavailability Across a Range of Molecular Weights
Abso
lute
Bio
avai
labi
lity
(%)
Molecular Weight (Da)7
The Enteris technology has enabledthe oral delivery of several peptidesand small molecules across a rangeof physical and chemical properties.
Bioavailability data from dogs
Peptelligence™ Clinical Development Pipeline
Candidate Preclinical Phase 1 Phase 2 Phase 3 NDA Sponsor
Ovarest™ (oral leuprolide tablet)
Tobrate™ (oral tobramycin tablet)
TBRIA™
CR845
CR845
GLP-1 analogs Undisclosed
GnRH Therapy Undisclosed
Peptides &Small
MoleculesUndisclosed
8
Type 2 Diabetes
Osteoarthritis
uUTI
Endometriosis
Enteris has conducted more than 25 pre-clinical fee-for-service feasibility programsNON-CONFIDENTIAL
Various
Osteoporosis
Pruritus
Cancer
9
Peptelligence™Patent Portfolio
Robust IP Protection
9 issued U.S. patents2 allowed U.S. patent applications
3 pending U.S. provisional patent applications
Key issued patents extend through at least 2030
29 issued Foreign patents5 pending Foreign patent applications
Enteris Clinical AssetsInnovative Oral Therapeutics for Women’s Health
10
Ovarest™ Oral Leuprolide Tablet for the Treatment of Endometriosis
11
Peptelligence™ Solution • Ovarest™ (oral leuprolide tablet), our leading product candidate isbeing evaluated for its potential to treat endometriosis
• Extensive market research and clinician feedback indicates thatdaily oral leuprolide tablet would offer patient friendly alternative tomonthly depot injections and drive Ovarest™ use early and moreoften
• Estimated at >$600M in the United States for endometriosis
Clinical Development • Crossover PK/food effect Phase 1 study completed in 14 healthyvolunteers
• Pre-study activities initiated for Phase 2a parallel group PK/PDstudy in 38 healthy volunteers
Need • 6 million U.S. women have endometriosis• Limited efficacy with oral and injectable hormonal contraception• LUPRON DEPOT® (leuprolide acetate for depot suspension) most
efficacious treatment; No oral formulation exists on the market
Ovarest™ Clinical Development Plan
12*This plan has incorporated FDA (DBRUP) recommendations per PIND Meeting 125004 held on Dec. 15, 2014.
Phase 1Crossover PK/Food Effect study in 14 healthy volunteers
3 Ovarest doses vs 1 mg SC
Phase 2a Parallel group PK/PD
study in 38 healthy volunteers
4 mg tablet QD 4 mg tablet BID
Leuprolide Depotfor 1 month
PD Endpoint: Estradiol Suppression
Phase 3Two parallel-group, double-blind studies
in women with endometriosis
Phase 2b Pilot efficacy study
in women with endometriosis
Study Completed Pre-study activities initiated
EOP2 Meeting
Tobrate™Oral Tobramycin Tablet for the Treatment of uUTI
13
Peptelligence™ Solution • Tobrate™ (oral tobramycin tablet) is being evaluated for its potentialto treat uUTI
• Tobramycin is an ideal candidate for uUTI as it concentrates in theurine after dosing – enables lower dose
• Low dose / short duration improves safety profile• Tobrate™ is commercially viable, with the potential to reach more
than $400M in sales, even as primarily a second line agent
Clinical Development • Currently in randomized, double-blind SAD/MAD PK Phase 1 studyin 24 healthy volunteers; data expected early Q1 2017
• Population PK modeling with microbial susceptibility data todetermine target attainment (POC: greater than 90%)
Need • Uncomplicated urinary tract infections (uUTI) are highly prevalent,affecting 10 million U.S. women each year
• Currently available first-line therapies are becoming increasinglyineffective due to antibiotic resistance
• Tobramycin, which has minimal resistance issues, is available in avariety of dosage forms but no oral formulation exists on the market
Tobrate™ Clinical Development Plan
14
Phase 1Randomized, double-blind SAD/MAD PK
study in healthy volunteers
N=24
3 Tobrate™ doses vs Tobramycin IV
Target Attainment Modeling
Population PK StudyNorth American
Surveillance StudyEx vivo UBT study
Phase 3Pivotal Efficacy /
Safety Trial in 800-900 Patients with
Acute Cystitis
Option 1: Placebo controlled non-
standard superiority trial
Option 2: Active controlled standard non-inferiority trial
FDA Meeting
Dosing in 8/16
Partner Clinical AssetsProviding Advanced Oral Formulation Solutions to Build Long-Term, Strategic Partnerships
15
16
Peptelligence™Key Differentiators
Enteris BioPharmaPartners Receive
The only technology in the industry that has demonstrated broad
applicability, effectiveness, and scalability
Manufacturing expertise and infrastructure to scale production up to small commercial scale
The only technology with predictable performance: reliable estimation of likelihood of success based on API
physical-chemical properties
Peptelligence™ Clinical Trial / Commercial Tablet Manufacturing Capability
• GMP facility• Strong inspection history (no 483s
issued in last 3 FDA inspections)• Most recent inspection: Jan. 2016
• Manufacture of Phase 1 and 2 clinical trial material
• Developing capacity for 50-250kg commercial batches
• Dedicated R&D, process development, tableting and film-coating suites
• Full QA/QC
• Analytical development, release and stability
17
Tarsa Therapeutics & TBRIA™Overview
18
Peptelligence™ Solution • TBRIA™ employs our proprietary technology, allowing for once-daily oral delivery of calcitonin
• Provides a more convenient route of administration for patients andmay result in better patient compliance
Clinical Development • Phase 3 ORACAL trial showed TBRIA™ was superior to both nasalcalcitonin spray and placebo in increasing bone mineral densityafter 48 weeks
• NDA submitted in October 2015 for the treatment ofpostmenopausal osteoporosis in women greater than 5 yearspostmenopause when alternative treatments unsuitable
Need • Injectable and intranasal calcitonin has been used for the treatmentof osteoporosis for more than 35 years
• Osteoporosis patients either abandon or are reluctant to initiatetreatment due to medication interfering with their lives or side effectconcerns
Cara Therapeutics & Oral CR845Osteoarthritis and General Chronic Pain
19
Peptelligence™ Solution • Oral CR845 tablet formulation synthesized using our proprietaryPeptelligence™ technology platform
• Oral delivery of peripherally selective kappa opioid agonist haspotential to provide continuity of care for acute and chronic painpatients
Clinical Development • Positive Phase 2a for OA trial results reported in Q4 2015• Double-blind, placebo-controlled Phase 2b for OA trial initiated
September 2016
Need • Currently marketed opioids inhibit intestinal transit and carry a riskof causing addiction and life-threatening respiratory depression
• 79% of patients report adverse events from pain medications –most adverse events are opioid-related
• Significant need among osteoarthritis (OA) and general chronic painpatients for new treatment options
Cara Therapeutics & Oral CR845Phase 1b Study Data
• Confirmed Analgesic Exposure at 1mg-5mg Tablet Strength• Well Tolerated –No SAEs on Single or Repeat Dose (6 day b.i.d.)
20
Cara Therapeutics & Oral CR845Positive Top-Line Results in Phase 2a Osteoarthritis Study
21
5.0 mg Dose Group • 50% reported at least a 30% reduction in pain score at the end oftreatment period
• Integrated AUC analysis of overall NRS score indicated a significantreduction compared to lower doses (Wilcoxon Rank Sum Test:p=0.02)
• Pain score reduction accompanied by a significant reduction inmean rescue medication of approximately 80% (ANOVA: p=0.02)
• 59% of patients used no rescue medication in Week 2• Dose effectiveness was further supported by significant, dose-
related increases in the proportion of patients whose OA was "verymuch improved" or "much improved” (Cochran-Mantel-Haenszeltest, p=0.02, 2-sided)
Overall • Dose-related reduction in mean joint pain score (NRS) after two-weeks, ranging from -25% (0.25 mg) to -34% (5.0 mg)
• All four tablet strengths observed to be safe and well tolerated
Cara Therapeutics & Oral CR845 Uremic Pruritus
22
Peptelligence™ Solution • Oral CR845 tablet formulation synthesized using our proprietaryPeptelligence™ technology platform
Clinical Development • Phase 1 trial for pruritus initiated in October 2016 in hemodialysispatients
Need • Uremic pruritus (UP) is an intractable systemic itch condition thatoccurs with the greatest frequency and intensity in chronic kidneydisease
• Prevalence of UP to be approximately 40 percent of patients withend-stage renal disease (ESRD), with approximately 24 percent ofpatients reporting severe pruritus.
• Moderate-to-severe chronic pruritus has repeatedly been shown todirectly decrease quality of life, contribute to symptoms that impairquality of life (such as poor sleep quality), and is associated withdepression.
Enteris BioPharmaOverview
23
Internal Pipeline • Lead product candidate, Ovarest™ (oral leuprolide tablet), being evaluated in a Phase 2 clinical trial for its potential to treat endometriosis
• Tobrate™ (oral tobramycin tablet) is being evaluated in a Phase 1 clinical trial for its potential to treat uUTI
Clinical / Commercial Tablet Manufacturing
• Experienced clinical trial manufacturer to support our partners’ research and development needs.
• Supply of GMP clinical trial / commercial material, analytical development, and stability testing
Peptelligence™ PlatformProprietary, Cutting-Edge Oral Drug Delivery Technology
• Novel formulation technology enables oral delivery of molecules that are typically injected, including peptides and BCS class II, III, and IV small molecules
• Robust IP protection in the U.S. and abroad through 2030
Feasibility-to-Licensing Partnering Program
• Advanced oral formulation solution• Recent successes:
• Tarsa Therapeutics – NDA submitted for TBRIA™ in osteoporosis• Cara Therapeutics – Phase 2b initiated in 9/2016 in chronic pain
(osteoarthritis) and Phase 1 initiated 10/2016 in uremic pruritus
Thank You!