Developing clinical stage small molecule therapeutics to treat hormonal and reproductive system disorders

Forward-Looking StatementsThis presentation contains forward-looking statements and information regarding the future performance and actions of Repros Therapeutics Inc. (RPRX) that involve risks and uncertainties that could cause actual results and actions to differ materially. These risks include those discussed in this presentation and others that can be found in Repros Form 10-K for the year ended December 31, 2007 and in the subsequently filed Form 10-Qs, which contain additional important risk factors that could cause actual results to differ from its current expectations and from the forward-looking statements made in this presentation. RPRX is providing this information as of this date and does not undertake any obligation to update any forward-looking statements contained in this document as a result of new information, future events or otherwise. No forward-looking statement can be guaranteed and actual results may differ materially from those we project. The results of initial clinical trials do not necessarily predict the results of later-stage clinical trials. RPRX cannot guarantee that data collected from clinical trials of any product candidate will be sufficient to support FDA or other regulatory approval.

Repros Strategy

Focus on small molecule therapeutics for hormonal and reproductive system disorders that exhibit significant market potential and that are currently underservedLate stage development of highly differentiated drugsProellex for the treatment of female reproductive system disordersAcute anemia associated with uterine fibroidsChronic relief of uterine fibroid symptomsChronic relief of the symptoms associated with endometriosisAndroxal for the treatment of endocrine disordersTreatment of Type II Diabetes in men with hypogonadotropic hypogonadism Fertility preservation/improvement in treatment of 2 hypogonadismProven track record of efficient and rapid clinical development

Repros Market OpportunityProellexUterine fibroid anemia$140 million/yearUterine fibroid symptoms$1.75 billion/yearEndometriosis symptoms$1.70 billion/year

AndroxalFertility preservation$250 million/yearType II Diabetes$>1 billion/year2 hypogonadism ex-US$100 million/year

Total Potential Market~$5.0 billion/year

Repros Pipeline

Proellex

Proellex OverviewNew class of selective progesterone receptor modulator (SPRM)Suitable for chronic and acute indicationsPotential significant advantages over existing GnRHa standard of careNo loss of bone mineral density in clinical trialsNo chronic drug treatments availableExcellent, long-term IP protectionUS issued composition of matter patent to 2017Eligible for Hatch-Waxman extensionPotential use applications with life to 2027Worldwide exclusive rightsIn-licensed from NIHIncludes 43 additional compounds

Uterine FibroidsLarge Underserved MarketMost common tumor of the female reproductive tractHeavy bleeding / anemiaAbdominal pressure / pain / urinary frequencyConservative Estimate, 15% of women of reproductive age with symptomatic uterine fibroidsPotentially 26,000,000 women in US, Japan, France, Germany, Italy, Spain, & UK with symptomatic fibroidsEstimated 700,000 severe cases currently requiring surgery or radical treatment in large market countriesMean age of women seeking UF treatment, 39Potential years on therapy, 10Uterine Fibroids regress when a woman reaches menopauseIf only 25% of severe population use drug option$1,750,000,000/yr Market ($140 million for anemia)

Key Symptom Driving Women to Seek Therapyfor Uterine FibroidsExcessive Menstrual BleedingUS Phase IIb(n=127)P80Basis for Commencement of US Phase III StudiesProellex stops bleeding

Basis for Anemia IND and Ongoing Phase III StudiesChange in Hemoglobin Levels in Anemic Patients (

Phase 2 Uterine Fibroid Trial UFSQOL (Co-primary endpoint in Phase III)UFSQOL Uterine Fibroid Symptom Survey High score > severity Month 3 significance values v.s. placebo; 25 mg p

EndometriosisEpithelial & stromal endometrial cells outside the uterine cavityPelvic and back painInfertilityPain during sexSevere menstrual cramps5% of reproductive-age women more that are undiagnosed71-87% of women with chronic pelvic pain25-40% (2-4 million) infertility cases could be due to endometriosis53% of teenagers with crampsUnmet medical need chronic condition, poor treatment optionsLupron, OCs, Danazol, laparoscopic proceduresHigh recurrence rates after treatment

US Phase 2 Endometriosis studyMESSS QuestionnaireUS Phase II Endpoint

US Results for End of Phase II MeetingModified Endometriosis Symptom Survey Total MESS Score Max.=15 (Last Observation Carried Forward)Total possible score = 1515 patients in placebo group and 14 each in 25 & 50 mg No statistical difference between 25 & 50 mgAfter week 4 all p values < 0.01

US Results for End of Phase II MeetingModified Endometriosis Symptom Survey Patient Reported Outcomes Total Scores (Last Observation Carried Forward)Total possible score =915 patients in placebo group and 28 in 25 & 50 mg combinedNo statistical difference between 25 & 50 mgP=0.007P

US Results for End of Phase II Meeting Modified Endometriosis Symptom Survey Dysmenorrhea (Painful Menses) (Last Observation Carried Forward)Total possible score =315 patients in placebo group and 28 in 25 & 50 mg combinedNo statistical difference between 25 & 50 mgP=0.0002P

US Results for End of Phase II Meeting Modified Endometriosis Symptom Survey Deep Dyspareunia (Painful Sex) (Last Observation Carried Forward)Total possible score =315 patients in placebo group and 28 in 25 & 50 mg combinedNo statistical difference between 25 & 50 mgP=NSP=0.0056P=0.0005P=0.004

US Phase II ResultsModified Endometriosis Symptom Survey Non Menstrual Pelvic Pain (Last Observation Carried Forward)Total possible score =315 patients in placebo group and 28 in 25 & 50 mg combinedNo statistical difference between 25 & 50 mgP=NSP=NSP=0.014P=0.003

US Phase 2 Endometriosis studyAnalgesic Use (narcotic & non narcotic)Analysis based on Patients last observation carried forwardp=.0025 50 vs Pbop=.0078 25 vs Pbo

Study Dropouts50 mg (5 patients)2-Lost to follow up2-Non compliance with study protocol1-Found to be Osteopenic on day of first dose25 mg (7 patients)2-elected hysterectomy upon completion of study1-osteopenic, should not have been randomized1-preexisting condition of auto immune disorder, should not have been randomized1-endometrial stripe not measureable1-exacerbation of depression and anxiety (never dosed)1-non compliance, patient stopped taking drugPlacebo (14 patients)9-lost to follow up1-no diagnosis of endometriosis1-adverse event (burning throat when taking drug)2-lack of relief1-osteopenic, should not have been randomized.

US Phase II Endometriosis Study25 mg Patients Electing HysterectomySituations Leading to Election of Hysterectomy Open Label Study not available for dosing until March/April 09. Patients completed double blind study in Nov. 2008.

Hysterectomy to treat severe endometriosis is relatively common option (120,000 procedures in the US annually) Subject 1 was informed about the extension study (not yet dosing), but reported that due to her long history of endometriosis and severity of her condition she proceeded with the hysterectomy. This subject is now 36 years old.Subject 2 was informed about the extension study but withdrew after completing Visit 7. She did not have worsening symptoms, only that she did not want to go without medications. The subject recently obtained insurance, which enabled her to have the procedure. This subject is now 43 years old.

ProellexSafety ExperienceWell tolerated at all dosesNo observed QT effects at up to 4X maximum clinical dosePotential for break through vaginal bleeding significantly reduced by incorporating off-drug intervalsOpen-label extension study confirming positive impact of off-drug interval

Off Drug Interval Treatment Strategy4 Month Dosing Cycle4 Month Dosing Cycle4 Month Dosing CycleOff Drug Interval to allow for:MensesRefresh the endometriumExperience to date suggests menses returns in 25-35 daysReturn of symptoms

Continue as neededConcept has been accepted by the FDAas noted in End of Phase II meeting minutes

ProellexSummary of FDA meetingsFDA will entertain multiple label indicationsFirst NDA: Preoperative treatment of Anemia2nd NDA: Chronic treatment of symptoms associated with fibroids3rd NDA: Chronic treatment of symptoms of endometriosisInitial Phase III programs anemia and fibroidsInitiated Two 65-patient trials Anemia prior to surgery for fibroidsInitiated Two 75-patient trials Symptoms associated with uterine fibroidsOngoing Phase II endometriosis study (n=75)Interim results reportedOpen label extension studies as required to satisfy safety data baseInitiated 400 patient 2-cycle study with holiday until symptoms return (25mg or 50mg Proellex )Initiated 400 patient 3-cycle study with holiday until menses returns to satisfy FDA need for 200 patients for one year of dosingProtocols submitted to FDA for input Total pooled safety data base ( 1,500 patients) Phase I-III trials as part of submission

Proellex Market Opportunity Uterine fibroid anemia

Uterine fibroid symptoms

Endometriosis symptoms +$3.5 Billion/Year Market

Androxal

AndroxalTrans isomer of clomiphene citrateCis isomer opposes action and has increased side effect riskAntiestrogen that normalizes pituitary responsiveness in 2 hypogonadal menHighly statistically significant results in 6 month Phase III study showing restoration of pituitary responsiveness resulting in normalization of testicular function and testosterone levelsMultiple patents and patent applications including pure isomer composition

Androxal Regulatory Strategy & Development Status Ongoing Phase II incorporating FDA commentsPreservation of fertility and testicular function and normalization of testosterone in hypogonadal men of reproductive age

Based on FDA correspondenceSubmission of IND for Type II Diabetes

Impact of Androxal on Male FertilityBasis for Ongoing US Phase IIComparison of Means p=0.011Comparison of Median p=0.0045Estimated 1/3 of current T market ($750 million) are men of reproductive age32% of men in Repros study under age of 50Exogenous testosterone suppresses pituitary secretion of FSHFSH required for stimulation of sertoli cell spermatogenesisSuppressed FSH suppresses spermatogenesis as evidenced by reduction in testicular size

Ongoing Androxal Phase IIImpact on sperm function and testosterone levelsThree arm (n=24) open label study with active comparator (Testim) in hypogoandal men previously treated with testosterone8 men with 3 week washout followed by 25 mg Androxal for 6 months8 men with 3 month washout followed by 25 mg Androxal for 6 months8 men with 3 week washout followed by Testim for 6 monthsEndpointsChange in sperm function from baseline to months 3 & 6Change in pituitary hormones and testosterone from baseline to months 3 & 6

Impact of Hypogonadism on Insulin Sensitivity and Metabolic SyndromeAmerican Heart Association definition of Metabolic Syndrome

Elevated waist circumference, 40

Triglycerides, 150 mg/dl

Reduced HDL, < 40 mg/dl

Elevated Blood Pressure, 130/85

Elevated Fasting Glucose, 100 mg/dlP

Change in Serum GlucoseSubset of Men BMI>26, Glucose >99 (+50% patients studied)No significant change in Placebo or Androgel armsSignificant mean change in Androxal arm p

Recent and Upcoming Milestones & Goals 2Q07 Reported top-line Proellex Phase 2b fibroid data 3Q07 Commenced US Proellex Phase 2 endometriosis trial 3Q07 Reported non-pivotal Phase 3 Androxal data 1Q08 Submitted Anemia IND 1Q08 Commence Phase 3 registration trials for Anemia 1Q08 Report data from ongoing Proellex open-label fibroid trial 1Q08 Commence Phase 3 registration trials for fibroid symptoms 3Q08 Report interim Proellex Phase 2 endometriosis data 3Q08 Commence Phase 2b Androxal fertility preservation trial 2Q09 Request endometriosis end of Phase 2 meeting with FDA H209 Report Phase 3 Anemia registration trial top-line data H209 Report Phase 3 Fibroid registration trial top-line data H209 Commence Phase 3 registration trials for Endometriosis H209 Report Androxal Phase 2b fertility preservation trial H209 Submit Proellex Anemia indication NDA H210 Submit Proellex Chronic Fibroid indication NDA

Repros FundamentalsShares Outstanding15,174,904 (all common, no warrants)No Debt2006 Net Loss$14,195,000 2007 Net Loss $13,700,0002008 Net Loss (through 9/08)$19,300,000Unaudited Cash on 12/31/08 : approximately $19.4 million

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