IPR2015-01836
`CFAD V. UPENN
`PENN EX. 2045
`
`1 of 15
`
`Vice President, PPD Discovery
`
`Gail McIntyre, PhD
`
`Dapoxetine
`
`
`CFAD V. UPENN
`PENN EX. 2045
`
`1 of 15
`
`Vice President, PPD Discovery
`
`Gail McIntyre, PhD
`
`Dapoxetine
`
`
`
`IPR2015-01836
`CFAD V. UPENN
`PENN EX. 2045
`
`2 of 15
`
`•2003: PPD acquires from Lilly the patents for dapoxetine for
`•2000: PPD licenses dapoxetine to Alza
`
`development in the field of genitourinary disorders
`
`investigates drug as treatment for premature ejaculation
`
`•1998-1999: PPD licenses dapoxetine from Lilly and
`
`Program highlights
`Dapoxetine
`
`
`
`IPR2015-01836
`CFAD V. UPENN
`PENN EX. 2045
`
`3 of 15
`
`•The premature ejaculation is not due exclusively to the direct
`
`effects of a substance (e.g., withdrawal from opioids)
`
`•The disturbance causes marked distress or interpersonal
`
`difficulty
`
`frequency of sexual activity
`age, novelty of the sexual Partner or situation, and recent
`factors that affect duration of the excitement phase, such as
`the person wishes it. The clinician must take into account
`stimulation before, on, or shortly after penetration and before
`
`•Persistent or recurrent ejaculation with minimal sexual
`
`DSM IV diagnostic criteria for Premature Ejaculation (302.75):
`Dapoxetine
`
`
`
`IPR2015-01836
`CFAD V. UPENN
`PENN EX. 2045
`
`4 of 15
`
`1Laumann et al., JAMA 281: 537 (1999)
`
`Prevalence of Premature Ejaculation (PE) v
`
`Prevalence
`Dapoxetine
`
`18
`11
`9
`7
`(5 million)
`ED
`[% within each age group]1
`Erectile Dysfunction (ED)
`
`31
`28
`32
`30
`(20 million)
`PE
`
`50-59
`40-49
`30-39
`18-29
`(# Affected in US)
`Age
`
`
`
`
`
`IPR2015-01836
`CFAD V. UPENN
`PENN EX. 2045
`
`5 of 15
`
`•McCabe, "Intimacy and Quality of Life Among Sexually Dysfunctional Men..”
`"Quality of Life"
`emotional, and sexual intimacy and various aspects of
`
`•PE correlates with decreased levels of intellectual,
`
`J. Sex Marital Ther. 23: 276 ('97)
`
`•Rust et al., "Marital Problems and Sexual Dysfunction..." Br.J. Psychiatry
`marriage
`•PE correlates significantly with male perception of poor
`
`152:629 ('88)
`
`•Kockott et al., "Symptomatology and Psycholgical Aspects of Male Sexual
`
`Inadequacy...." Archives Sex. Behav. 9:457 ('80)
`•Sexual avoidance, anxiety, inadequacy
`
`Consequences of PE
`Dapoxetine
`
`
`
`IPR2015-01836
`CFAD V. UPENN
`PENN EX. 2045
`
`6 of 15
`
`•Behavioral - clumsy, painful and poorly effective for long term
`
`•Master's and Johnsons - pause-squeeze technique
`•Seman's - pause technique
`management
`
`•Pharmacological - none approved
`
`•Antidepressants
`
`Current therapies
`Dapoxetine
`
`
`
`IPR2015-01836
`CFAD V. UPENN
`PENN EX. 2045
`
`7 of 15
`
`and sexual intimacy and various aspects of "Quality of Life"
`•PE correlates with decreased levels of intellectual, emotional
`
`•Drug action addresses important regulator of sexual function
`
`•PE correlates significantly with male perception of poor
`•Sexual avoidance, anxiety, inadequacy
`•positive and negative regulation of sex
`•libido, arousal, orgasm
`
`marriage
`
`Rationale for use in PE
`Dapoxetine
`
`
`
`IPR2015-01836
`CFAD V. UPENN
`PENN EX. 2045
`
`8 of 15
`
`Source: R&D Focus
`
`*PoC study did not demonstrate delayed time to ejaculation; studies continue
`Pfizer
`VIVUS
`
`II
`IIa*
`
`PoC
`IIa
`
`Phase
`
`PDE5
`(Alprostadil cream/anesthetic)
`Topical: prostaglandin
`SSRI
`
`NexMed
`Enhance/Barr
`
`Class of Drug
`
`Company
`
`Competition
`Dapoxetine
`
`
`
`IPR2015-01836
`CFAD V. UPENN
`PENN EX. 2045
`
`9 of 15
`
`•Dapoxetine has PK profile favorable for p.r.n. dosing
`
`•Sex is intermittent and spontaneous, thus treatment should:
`
`•Have rapid onset of action
`•Be conducive to “as needed” dosing
`
`Competitive advantage
`Dapoxetine
`
`
`
`IPR2015-01836
`CFAD V. UPENN
`PENN EX. 2045
`
`10 of 15
`
`•Secondary endpoints: global satisfaction and PE
`•Primary endpoint: ejaculation latency
`
`questionnaire
`
`HCl in the treatment of premature ejaculation
`cross-over study of the safety and efficacy of dapoxetine
`•Phase II, double-blind, randomized, placebo-controlled,
`
`Proof-of-concept study
`Dapoxetine
`
`
`
`IPR2015-01836
`CFAD V. UPENN
`PENN EX. 2045
`
`11 of 15
`
`Post-Treatment
`
`PE Patients
`
`Pre-Treatment
`
`PE Patient
`
`15% 15%
`
`Increase
` 3 Fold
`
`~~
`
`41% 41%
`
`0%
`
`10%
`
`20%
`
`30%
`
`40%
`
`50%
`
`Sexual Satisfaction Rating of “Good” or “Very Good”
`Sexual Satisfaction Rating of “Good” or “Very Good”
`
`Percent of Patients Reporting
`Percent of Patients Reporting
`
`Improves satisfaction rating
`Dapoxetine
`
`
`
`IPR2015-01836
`CFAD V. UPENN
`PENN EX. 2045
`
`12 of 15
`
`•Dapoxetine appears to be generally well tolerated based on
`improvements in subjects with PE following p.r.n. dosing
`•Dapoxetine produces statistically and clinically significant
`
`clinical and preclinical data available at this time
`
`Conclusions from Phase IIa study
`Dapoxetine
`
`
`
`IPR2015-01836
`CFAD V. UPENN
`PENN EX. 2045
`
`13 of 15
`
`•Safety profile remains the same
`•Program is on schedule
`
`•Additional safety studies have been conducted
`•Involves 2,400 patients
`•Phase III studies are in progress
`
`Program at ALZA
`Dapoxetine
`
`
`
`IPR2015-01836
`CFAD V. UPENN
`PENN EX. 2045
`
`14 of 15
`
`•No products currently approved
`
`•Competition weak
`
`•Affects 25-35% of men ages 18-64 years
`•Large, unsatisfied patient population
`
`Potential market
`Dapoxetine
`
`
`
`IPR2015-01836
`CFAD V. UPENN
`PENN EX. 2045
`
`15 of 15
`
`1Laumann et al., ('99); 2Reading and Weist ('84)
`
`•60% of “Western men” (i.e., 55 million in US) “wish to
`
`delay ejaculation”2
`
`•21% incidence PE1- 20 million have clinical diagnosis of
`
`•74% of our patients rated severity as "extreme"
`•5-fold greater recruitment rate than we expected
`PE
`
`Treatable population: dapoxetine
`Dapoxetine
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