Transcript Document
Giuseppe Remuzzi Prevention of progression and remission/regression strategies of chronic renal diseases: can we do better now than 5 years ago? Bellagio, March 16, 2004 1 There are 1,065,000 people on dialysis worldwide 90 % of them live in North America, Japan, and Europe, whose population is less than 20 % of world population 2 PREDICTED DIALYSIS COST OF APPROXIMATELY $ 1.1 TRILLION FOR THE COMING DECADE Ten year medical costs of dialysis population $ ( billions) 1200 1000 800 600 400 200 0 1981-1990 1991-2000 2001-2010 Lysaght et al., J Am Soc Nephrol, 2002 3 1,000,000 deaths 4 PROGRESSION OF RENAL FAILURE IN 9 DIABETICS 80 1/Cr x 10 3 (µmol/l) 60 40 20 0 0 10 20 30 40 50 Time (months) Jones et al., Lancet, 1979 5 700 DEATH IN * 600 (mg/24 hrs) 500 400 300 200 100 ** Percentage of glomeruli affected by sclerosis 0 Control 100 UNx UNx + Lis * Control UNx + Lis 100 80 Survival (%) Urinary Protein Excretion ACE INHIBITION PREVENTS RENAL FAILURE AND UNINEPHRECTOMIZED MWF/ZTM RATS 60 40 20 ** 80 60 40 20 UNx 0 0 Control * p < 0.05, **p < 0.01 vs control UNx UNx + Lis 0 3 6 9 12 15 Time (months after UNx) Remuzzi et al., Kidney Int, 1995 6 EFFECT OF ACE-I THERAPY ON RISK OF DEATH IN NON-DIABETIC CHRONIC RENAL DISEASE Risk of death Patients - Zucchelli et al., 1992 121 - Kamper et al., 1992 70 - Brenner et al., 1993 112 - Toto et al., 1993 124 - van Essen et al.,1994 103 - Hannedouche et al., 1994 100 - Bannister et al., 1994 51 - Hansson et al., 1995 260 - Ihle et al., 1996 - Maschio et al., 1996 Risk Ratio & C.I. 60 70 583 Pooled Risk Ratio (95% CI) - OVERALL 1594 1.24 (0.55 - 2.83) ACE-I better 0.01 0.05 0.2 ACE-I worse 1 5 20 Patients with proteinuria (%) Author, year 50 % 35 % 30 15 % 0 < 0.5 100 0.5 - 3 ≥3 Proteinuria (g/24 h) Giatras et al, J Am Soc Nephrol, 1997 7 REIN CORE Rate of GFR decline according to base-line proteinuria - Interim analysis on 177 patients p=0.001 1.0 0.67±0.08 0.5 0.25±0.08 (ml/min/month) p=0.001 Rate of GFR decline (ml/min/month) Rate of GFR decline 1.0 0.89±0.11 0.39±0.10 0.5 0 Conventional Ramipril 0 STRATUM - 1 STRATUM - 2 U. Prot. < 3 g/24 h U. Prot. ≥ 3 g/24 h Kidney survival: Conventional 54 % Ramipril 77 % GISEN Group, Lancet, 1997 8 Conventional Ramipril % patients with doubling of baseline creatinine or ESRF 1.6 (ml/min/month) Mean rate of GFR decline REIN CORE 1.4 1.2 1.0 0.8 0.6 0.4 70 60 50 40 30 20 0.2 10 0 0 3 - 4.5 4.5 - 7 ≥7 Baseline proteinuria (g/24 h) 3 - 4.5 4.5 - 7 ≥7 Baseline proteinuria (g/24 h) GISEN Group, Lancet, 1997 9 AN ARTIFICIAL NEURAL NETWORK TO MODEL INDIVIDUAL OUTCOME OF PATIENTS WITH CHRONIC NEPHROPATHIES ON THE BASIS OF DATA FROM THE REIN STUDY Besides serum creatinine, the model identified proteinuria and Ca*P product as the strongest predictors of ESRD 10 RISK OF PROGRESSION TO ESRD OVER 20 MONTHS FOLLOW-UP IN PROTEINURIC CHRONIC NEPHROPATHIES 80 Predicted risk in 3 explicative cases % 60 40 20 1.2 1.9 24.3 2.1 3.9 35.1 3.5 5.2 37.2 Serum creat mg /dl Proteinuria g /24 h CaxP mg2/dl2 0 11 3 MONTHS PROTEINURIA REDUCTION PREDICTS LONG-TERM GFR DECLINE The REIN study - 0.9 Ramipril Overall Conventional > 3 gr/24 h - 0.7 3 years GFR (ml/min/month) - 0.8 - 0.6 -0.5 - 0.4 -0.3 -0.2 - 20 0 20 40 proteinuria * ( percent change vs .baseline) 3 months * Corrected for GFR Perna et al., J Am Soc Nephrol, 2000 12 1 - 3 gr/24 h 40 Placebo - 0.7 - 0.8 0.9 - 20 -0.3 - 0.4 > 3 gr/24 h 40 3 months ( percent change vs .baseline) Overall 0 - 0.2 proteinuria * Ramipril 20 3 months (percent change vs. baseline) proteinuria * CORRELATION BETWEEN CHANGES IN PROTEINURIA AND GFR DECLINE 20 0 - 20 -0.2 -0.3 * Corrected for GFR - 0.4 -0.5 - 0.6 GFR (ml/min/month) 3 years Perna et al., J Am Soc Nephrol, 2000 13 6 MONTHS PROTEIN/CREATININE RATIO REDUCTION PREDICTS RENAL AND CARDIOVASCULAR EVENTS The RENAAL study Hazard ratio (95 % C.I.) ESRD CV events Heart failure Increased risk Decreased risk 0.2 0.4 0.6 0.8 1 1.2 RENAAL Study group, 2002 14 PROTEINURIA AND RISK OF DEVELOPING ESRD Community-based screening in 106,177 general population Cumulative incidence of ESRD (%) Follow-up: 17 years 16 14 12 10 8 6 4 2 0 Proteinuria Number of screened Number of ESRD - + + 2+ >3+ 86,253 10,000 4,007 1,072 357 185 38 55 76 55 Iseki et al., Kidney Int, 2003 15 RISK OF ESRD: PREDICTIVE VALUE OF BASELINE GFR AND PROTEINURIA 1993 mass screening conducted by the Okinawa General Health Maintenance Association (OGHMA) Subjects 95,255 Inclusion criteria > 20 years of age GFR > 15 ml/min Baseline parameters Dipstick proteinuria Calculated GFR (Cockcroft-Gault method) Follow-up 7 years End point ESRD Iseki et al., J Am Soc Nephrol, 2003 16 Cumulative Incidence of ESRD per 1,000 screened in 7 years Fig3 80 Proteinuria (+) Proteinuria (-) 60 40 20 0 15.0-57.1 57.2-77.6 77.7-102.6 ≥102.7 Total GFR, ml/min/1.73m2 Proteinuria (+) Number of screened Number of ESRD 1,125 84 811 11 717 7 800 6 3,453 108 21,872 22 22,254 18 22,312 1 22,229 3 88,667 44 Proteinuria (-) Number of screened Number of ESRD 17 EFFECTS OF LOSARTAN ACCORDING TO RACE: Post-hoc analyses of the RENAAL study Region n° Primary end point p (Doubling s. creat, ESRD or death) Hazard ratio (95 % C.I.) Asian 252 0.024 Black 230 0.94 White 734 0.07 Hispanic 277 0.99 19 0.76 1,261 0.18 Other Overall Losartan worse Losartan better 0.25 0.5 0.75 1.0 1.25 1.5 The whole effect of Losartan was fully driver by Asian patients 18 1-YEAR PROTEINURIA REDUCTION IN TYPE 2 DIABETICS ENROLLED IN THE RENAAL STUDY ACCORDING TO RACE ASIA Non-ASIA n = 252 n = 1,261 Median (I.Q. range) proteinuria reduction vs baseline (%) 0 -5 -10 -9 (-51 to 40) -15 -20 -19 (-56 to 36) p = 0.03 (ANCOVA) 19 Baseline proteinuria p Reduced Outcome proteinuria improved (alb/creat g/g) Risk reduction (95 % C.I.) Asian 1.535 Non Asian 1.167 YES YES 0.016 NO NO 0.27 YES NO NO NO 0.59 0.35 Increased risk Decreased risk -75 -50 -25 1 25 50 75 20 BASELINE CHARACTERISTICS OF ASIAN AND NON-ASIAN PATIENTS OF RENAAL STUDY p Asian Non-Asian (257) (1256) 60+7 60+7 0.72 MAP (mmHg) 102+11 106+11 <0.005 BMI (Kg/m2) 25+4 31+5 <0.0001 Age (yrs) 21 45 Ramipril Ramipril GFR = -0.44 ± 0.54 (ml/min/month) GFR 40 GFR = -0.10 ± 0.50 35 30 GFR = -0.81 ± 1.12 GFR = -0.14 ± 0.87 25 Conventional CORE Ramipril FOLLOW-UP Ruggenenti et al., Lancet, 199822 0,10 ml/min/month 23 Regression 16 patients with stable GFR 10 patients with increasing GFR 90 90 80 80 70 70 GFR (ml/min/month) GFR (ml/min/month) Remission 60 50 40 30 60 50 40 30 20 20 10 10 0 0 0 10 20 30 months 40 50 60 0 10 20 30 40 50 60 months Slopes refer to 26 patients on continuated Ramipril treatment since randomization who had at least 6 GFR measurements (≥ 3 on Core and ≤ 3 on Follow-up study) 24 RELATIONSHIP BETWEEN REMISSION/REGRESSION BREAKPOINT CHANGES IN PROTEINURIA Post hoc analyses of the REIN study Remission Regression n = 16 n = 10 AND POST- - 20 (%) Proteinuria reduction vs pre-breakpoint values 0 -31 % - 40 -52 % - 60 The further improvement in GFR during continued ramipril therapy was always associated with further proteinuria reduction The extent of GFR amelioration was associated with the extent of proteinuria reduction Ruggenenti et al., J Am Soc Nephrol, 1999 25 REGRESSION OF THE DISEASE IN PATIENTS ON CONTINUED RAMIPRIL 50 GFR (ml/1.73 sqm) 40 30 * 20 Y1 = - 0.3291x + 44.794 10 Y2 =0.387x + 19.677 p (y1 vs y2 ): < 0.01 (F-test) * Y= 0.0092x - 0.6033x2 + 45.586 0 0 6 12 18 24 30 36 42 48 54 months 26 EVIDENCE FOR GLOMERULAR CAPILLARY REGENERATION AND REABSORPTION OF SCLEROSIS AREAS 100 MWF 60 w 80 Number of Glomeruli (%) 60 100 40 MWF 50 w 80 20 60 0 40 <25% 25-50% 50-75% >75% 100 MWF 60 w + LIS 20 0 0% 80 0% <25% 25-50% 50-75% >75% 60 40 20 0 Remuzzi et al., J Am Soc Nephrol, 2003 0% <25% 25-50% 50-75% >75% 27 CAN WE DO BETTER? protein traffic Intensify blood pressure control Up-titrate ACE inhibitor dose Combine with other antiproteinuric agents - Non-dihydropyridinic Ca-channel blockers - Ang II receptor blockers - Aldosterone antagonists Vasopeptidase inhibitors consequences of protein traffic Drugs targeted to inflammatory or vasoactive genes which are up-regulated by protein reabsorption - ET-1 receptor antagonists - TGFb inhibitors - Lipid lowering agents 28 THE EFFECT ON PROTEINURIA AND BLOOD PRESSURE OF INCREASING DOSES OF ACE INHIBITORS 24 h Proteinuria* M.A.P.* y=-1. 23x - 12. 07 r =-1.23; p<0. 02 vs. no treatment (%) 0 +20 -10 +10 -20 0 -30 -10 -40 -20 -50 -30 -60 -30 0 5 10 15 20 Ramipril dose (mg/day) 0 5 10 15 20 Ramipril dose (mg/day) * No correlation betw een proteinuria and BP changes 29 THE COURSE OF THE EFFECT OF ANG II ANTAGONISM ON BLOOD PRESSURE AND URINARY PROTEIN EXCRETION Blood pressure Urinary protein excretion Gansevoort et al., Kidney Int, 1994 30 Changes vs. basal (%) EFFECTS OF UP-TITRATING MEMBRANOUS NEPHROPATHY LISINOPRIL IN + 40 + 30 + 20 Serum Albumin + 10 0 - 10 - 20 - 30 LDL Cholesterol 0 10 20 30 40 10 0 Lisinopril dose (mg/day) Ruggenenti et al., Circulation, 2003 31 DUAL RENIN-ANGIOTENSIN SYSTEM BLOCKADE IS HIGHLY EFFECTIVE TO IN NON-DIABETIC PROTEINURICS 9 non-diabetic renal patients (6 weeks treatment per dose) Change of proteinuria (%) 0 -25 Losartan -50 -75 Lisinopril Combined -100 0 50 100 150 50 - 150 0 10 20 40 10 - 40 Laverman et al., Kidney Int, 200232 EFFECTS ON PROTEINURIA OF 8 WEEKS COMPARABLE BLOOD PRESSURE CONTROL ACHIEVED BY COMBINED THERAPY IN 23 PATIENTS WITH CHRONIC NON-DIABETIC NEPHROPATHIES 10 BENAZEPRIL (20 mg/day) VALSARTAN (160 mg/day) Percent change from baseline 0 BENAZEPRIL + VALSARTAN (10 + 80 mg/day) -10 -20 -30 -40 24 hrs Uprot excretion MAP -50 -60 p = 0.022 p = 0.024 -70 p = 0.002 Campbell et al., 2002 33 Dextran Fractional Clearance 1.0 * * 0.1 * * * * * ** * ** ** ** ** ** ** * 0.01 Baseline * 22 30 38 46 54 62 70 38 ** Basaline ** ** Valsartan 22 30 ** ** Baseline * Benazepril ** ** ** 46 54 62 ** Benazepril + Valsartan * 70 ** ** * 22 30 38 46 54 62 70 Molecular radius (Å) Dextran clearance studies found no differences in size selective properties of the membrane but more reduction in renal vascular resistance (p = 0.046) in combination therapy compared to each drug alone Campbell et al., 2002 34 Patients without events * (%) COOPERATE study: results 100 Combination Losartan Trandolapril 80 60 40 20 0 0 6 12 18 24 30 36 Months after randomisation * ESRD and doubling of serum creatinine Nakao et al., Lancet, 2003 35 800 Treatment for 10 months (start treatment at 2 months) (mg/day) Urinary protein excretion SEVERE PASSIVE HEYMANN NEPHRITIS (UNINEPHRECTOMY) 600 * 400 200 * 60 (%) Glomerulosclerosis 0 80 40 * * 20 * Vehicle Lisinopril Lis + AII-RA Lis + AII-RA +Cerivastatin Control Zoja et al., J Am Soc Nephrol, 2002 36 EDITORIAL J Am Soc Nephrol 13:3024 - 3026, 2002 The Next Treatments of Chronic Kidney Disease: If We Find Them, can We Test Them? THOMAS H. HOSTETTER National Institute of Health, National Institute of Diabetes and Digestive and Kidney Diseases, Bethesda, Maryland 37 REMISSION CLINIC Start low-dose sodium diet Add low-dose ACE i or AII RA Up-titrate ACE i or AII RA to max tolerated dose Add a diuretic Add a low dose of another antiproteinuric agent K < 5.5 mEq/l K > 5.5 mEq/l Add AII RA or ACE i Up-titrate AII RA or ACE i to maximum dose Add non-dihydropyridine CCBs (Verapamil/Diltiazem) Up-titrate non-dihydropiridine CCBs to max tolerated dose Up titrate concomitant antihypertensive agents to achieve the maximum tolerated blood pressure reduction Add a lipid lowering agent Ruggenenti et al., Lancet, 2001 38 FULL RESPONDERS (n=19) - Full remission of nephrotic syndrome (U.prot. <1g/24 h) - Stable s. creatinine over 4 years 5 Remission clinic 4 (g/24 hours) 3 4 2 2 1 0 0 - 10 Serum creatinine 6 (mg/dl) Urinary protein excretion 8 0 10 20 months 30 40 50 39 PARTIAL RESPONDERS (n=7) - Partial remission of nephrotic syndrome - s. creat increase < 0.2 mg/dl/year Remission clinic 5 (g/24 hours) 6 3 4 2 2 Serum creatinine 4 (mg/dl) Urinary protein excretion 8 1 0 -10 0 0 20 10 30 40 months 40 REMISSION CLINIC Targets of the multidrug approach: Blood pressure Proteinuria LDL LDL + VLDL HbA1c < 120/80 mmHg < 0.3 g/24 h < 100 mg/dl < 130 mg/dl < 7.5 % (diabetics) Ruggenenti et al., Lancet, 2001 41 OUTCOMES OF 160 TYPE 2 DIABETICS WITH MICROALBUMINURIA ACCORDING TO MULTIFACTORIAL OR CONVENTIONAL THERAPY Relative risk (95 % C.I.) Fatal and non-fatal CV events Nephropathy Retinopathy Multifactorial therapy better 0.0 0.5 Multifactorial therapy worse 1.0 1.5 2.0 Gaede et al., N Engl J Med, 2003 42 When to start, why never stop 43 INCIDENCE OF ESRD IN 352 PATIENTS WITH PROTEINURIC, CHRONIC NEPHROPATHIES ACCORDING TO TREATMENT AND TERTILES OF BASAL GFR Incidence of ESRD (%) 70 60 p < 0.05 60.0 % 50 40.4 % 20 10 21.4 % Ramipril 30 Conventional 40 p < 0.01 13.4 % 10.9 % 0.0 % 0 Lowest Middle Highest (10.5 - 32.6 ml/min) (32.6 - 50.8 ml/min) (50.8 - 101.0 ml/min) Ruggenenti et al., J Am Soc Nephrol, 2002 44 1998 - 2010 PREDICTED ESRD PREVALENCE AND CUMULATIVE SAVINGS FOR DIFFERENT DEGREES OF GFR REDUCTIONS ESRD 7.56 65,000 0 661,330 615,767 60,000 55,000 -10 % 50,000 466,438 45,000 -30 % 40,000 - 10 % - 30 % 10 20 18,56 30 40 50 60 60,61 35,000 2000 GFR reduction* Prevalence projections Costs saved ($ billion) Prevalence Predicted GFR (ml/min/yrs) 70 2005 2010 * Predicted for patients with basal GFR ≤ 60ml/min Hariprasad et al., Am J Kidney Dis, 2002 45 GFR (ml/min/month) GFR DECLINE ACCORDING TO DIFFERENT UNDERLYING RENAL DISEASE 1.2 Conventional Ramipril 1.0 0.8 0.55±0.13 0.6 0.53±0.09 0.49±0.11 0.36±0.09 0.4 0.31±0.09 0.31±0.07 0.2 0 Primary Glomerular IgA Nephropathy Nephrosclerosis -35 -37 Disease % GFR -42 reduction vs control Ruggenenti et al., Am J Kidney Dis, 2000 46 DEVELOPMENT OF A LOW COST “POLYPILL” TO PREVENT RENAL PROGRESSION AND CARDIOVASCULAR EVENTS • A single combination low cost pill containing six active components, including aspirin, a statin, three antihypertensive agents (a thiazide, a b-blocker, an ACE inhibitor) at half standard dose, and folic acid has been proposed for the prevention of cardiovascular disease Wald and Law, British Med J, 2003 47 Statin Aspirin ACE inhinitors The superpill could be valuable also for patients with chronic nephropathies to limit both renal and cardiovascular events 48 A LOW COST POLYPILL COULD USE GENERIC COMPONENTS Generic drugs are not subject to patent protection This formulation may not have the lowest rate of adverse effects, but even if about 10% of people were intolerant of the formulation it would still have considerable public health merit 49 So far, treatment of renal patients has been aimed to limit or prevent progression to ESRD 50 ANNUAL ESRD AND MORTALITY IN TYPE 2 DIABETICS WITH OVERT NEPHROPATHY 25 (%) ° 20 15 ? 10 * 5 0 Mortality ESRD Estimate from the °UKPDS and the *RENAAL studies Adler et al., Kidney Int, 200351 Preventing nephropathy is more important than retarding progression 52 PROJECTED CHANGES OF ISCHEMIC HEART DISEASE MORTALITY WORLDWIDE (1990 to 2020) 5000 Deaths (x 1000) 4500 DEVELOPING COUNTRIES 4000 3500 3000 2500 2000 1500 1000 500 0 DEVELOPED COUNTRIES 1990 2020 Yusuf et al. Circulation 2001 The obstacle in providing adequate health care to millions of people in poor countries are multiple - Poor infrastructures - Famine and malnutrition - Cultural attitudes - Inadequate public health systems - War 54 However, lack of access to essential drugs is a most striking aspect that underlines dramatically the existence of two different world 55 THE KIDNEY HELP TRUST PROJECT IN INDIA 25,000 people were screened for high blood pressure, diabetes, chronic kidney disease in the region of Tamil Nadu (India) The screening campaign was conducted by 6 trained social workers and 2 doctors India Tamil Nadu Patients with high blood pressure, diabetes or kidney diseases were put on cheap medications and followed - COST OF 1 YR OF THE PROJECT - COST PER PATIENT - PER CAPITA HEALTH EXPENDITURE $ $ $ 6,200 0.27 7.7 IN INDIA Mani, Kidney Int, 2003 56 The community programme of mass screening and free drug therapy, reported from India would not be sustainable if replicated across the whole of India 57 STARTING TO WORK FOR A LARGE-SCALE PREVENTION PROGRAM OF ESRD IN MOLDOVA MOLDOVA Chisinau Bergamo 4,762,000 population 33,700 Km2 Income per month: 70 $ Network between existing health care structures under the coordination of the Republican Clinical Hospital Chisinau Large--scale screening Intervention treatment Continuous education Health Authorities Mario Negri Institute Activation of a 4 yr program Moldova Society of Nephrology Igor Codreanu ISN-COMGAN 58 VIRTUAL NETWORKS OF EXCELLENCE TO LINK THE SCIENTIFIC TALENTS OF ENTIRE REGIONS Virtual networks of excellence are based on research programs jointly sponsored and conducted by research institutes in different geographical locations InterAcademic Council, 2004 59 CREATING AUTONOMOUS CENTERS OF EXCELLENCE TO ADDRESS LOCAL CHALLENGES Center of excellence - whether of local, national, regional, or international status should be created or planned in the near future in every developing nation in order for its science capacity to grown InterAcademic Council, 2004 60 THE EFFECT OF RAMIPRIL TRIALS ON ACE INHIBITOR PRESCRIBING IN ONTARIO (CANADA) REIN, HOPE All ACE inhibitors Ramipril 61 62 PERCENT PROFIT OF TOP COMPANIES IN EACH SECTOR 20 18,6 % 15 11,7 10 5,7 5 5,1 3,5 0 Pharmaceutical Telecom Airlines Chemicals Automobiles Fortune 500, 2000 63 PHARMACEUTICAL COMPANIES Year 2000 Percent of income 30 20 10 0 Marketing Research Fortune 500, 2000 64 INVESTMENT OF PUBLIC INSTITUTIONS ON INNOVATIVE DRUGS Pre-clinical studies Infrastructures Expertise - physicians - nurses - other professionals Angell, N Engl J Med, 2000 65 It is no unlikely that the preclinical research could account for as much as 20 to 25% of a company’s research budget Gerth and Stolberg, New York Times, 2000 66 It is becoming increasingly intolerable to know that innumerable lives are lost in poor countries only because relatively simple measures are not available because of their cost The contribution of pharmaceutical industry is fundamental to starting a new era of hope 67 A GLOBAL FUND FOR KIDNEY DISEASE 68 Pharmaceutical companies that profit from selling renoprotective drugs take the lead in establishing the fund The makers of drugs with renoprotective effects - not just ACE inhibitors and ARBs, but also blood pressure, diabetes, and cholesterol drugs - could donate 1 % of profit from sales of these drugs 69 WHAT TO DO WITH GLOBAL FUND? Further ISN prevention/education program and add primary care physicians and health professionals Begins centers of excellence with infrastructures so we can apply to agencies for funds Raise public awareness to renal survival 70 CORPORATE SOCIAL RESPONSIBILITY The one % solution: 1 % of equity 1 % of profit 1 % of employees’ paid hours are devoted to philanthropy Compassionate capitalism benefits the shareholders, the employees and the needy people Marc Benioff, Salesforce 71 72 Helping patients of a less developed country is a way to thank the contribution of so many volunteers 73 The industry's impact on public health is so great, and the subsidies and protections offered by governments so generous, that the industry should consider its social responsibilities 74 75 These slides are belonging to Giuseppe Remuzzi, M.D. Mario Negri Institute for Pharmacological Research, Bergamo, Italy. Using these slides is only authorized by mentioning the source 76 BASELINE PROTEINURIA PREDICTS THE RESPONSE TO RAS BLOCKADE Post-hoc analyses of the RENAAL study Alb/creat ratio n° Primary end-point (doubling, ESRD or death) (g/g) Hazard ratio (95 % C.I.) > 1.25 757 < 1.25 756 Overall 1,513 0.5 0.75 1.0 1.25 1.5 77 LESS NEED OF DIALYSIS FOR NON-DIABETIC AND DIABETIC RENAL DISEASE WITH RENIN-ANGIOTENSIN SYSTEM BLOCKADE REIN CAPTOPRIL RENAAL IDNT (n = 352) (n = 409) (n = 1,513) (n = 1,715) 0 Relative risk (%) - 10 - 20 - 20 % - 30 - 28 % - 40 - 50 - 45 % - 48 % 78 There is little doubt that ACE-I and ARBs have guaranteed substantial revenues, and their development costs have been largely paid off, since their sale is in the order of billions of dollars worldwide 79 INCIDENCE OF ESRD IN 1513 PATIENTS WITH TYPE 2 DIABETIC NEPHROPATHY ACCORDING TO TREATMENT AND TERTILES OF BASAL SERUM CREATININE (data from the RENAAL study) 40 30 10 Losartan 20 Placebo Incidence of ESRD (%) 50 0 S. Creatinine (mg/dl) 2.1 - 3.6 1.6 - 2.0 0.9 - 1.5 GFR (ml/min) 19 - 34 35 - 44 45 - 77 80 INCIDENCE OF HEART FAILURE IN 1513 PATIENTS WITH TYPE 2 DIABETIC NEPHROPATHY ACCORDING TO TREATMENT AND TERTILES OF BASAL SERUM CREATININE (data from the RENAAL study) p < 0.003 p < 0.01 25 21.3 19.3 15 13.4 11.3 11.0 5 9.0 Los 10 Placebo Incidence (%) 20 0 S. creat 2.1 - 3.6 Lowest 1.6 - 2.0 Middle 0.9 - 1.6 Highest TERTILES 81 mmHg Control 0.08 0.07 Diabetic 0.06 0.05 0.04 0.03 0.02 ** 400 * 300 200 100 0.01 Diabetes Pore radii distribution 0.09 63 mmHg Control 0.10 53 Urinary protein excre tion (mg/24 h) P GC 0 0.00 0 10 20 30 40 Pore radius (Å) 50 60 0 4 8 12 months Remuzzi et al., J Am Soc Nephrol, 1993 82 MAP (mmHg) 95 98 101 104 107 110 113 116 119 0 r = 0.69; p < 0.05 GFR (ml/min/year) -2 -4 -6 -8 -10 -12 -14 130/85 140/90 Diabetes Parving et al., Br Med J, 1989 Viberti et al., JAMA, 1993 Hebert et al., Kidney Int, 1994 Lebovitz et al., Kidney Int, 1994 Bakris et al., Kidney Int, 1996 Bakris et al., Hypertension, 1997 Untreated HTN Non-diabetes Klahr et al., N Engl J Med, 1993 Maschio et al., N Engl J Med, 1996 GISEN Group, Lancet, 1997 Bakris et al., Am J Kidney Dis, 2000 83 ACHIEVED BLOOD PRESSURE CONTROL IN MAJOR TRIALS ON NEPHROPATHY TYPE 2 DIABETES Trial SPB/DBP (mmHg) Study drug RENAAL 142/74 Losartan IDNT 142/84 Irbesartan IRMA 144/77 Irbesartan 84 In the 2010 Diabetes High blood pressure/chronic renal disease Need of dialysis 30 millions 80 millions 1 million CHINA 85 ANGIOTENSIN II PARTICIPATES TO THE DEVELOPMENT OF GLOMERULAR CAPILLARY HYPERTENSION Acute infusion of Ang II in normal rats raises intraglomerular capillary pressure Myers et al., Circ Res, 1975 Following 5/6 nephrectomy in rats endogenous Ang II local activity increases Mackie et al, Kidney Int, 2001 86 RENAAL Reduction of Endpoints in NIDDM with the AII Antagonist Losartan ESRD - 1513 type 2 diabetes 30 - Alb/Cr ratio >300 mg/g, - S Creat 1.3-3.0 mg/dL, % with event - Age 31-70 years P 20 Risk Reduction: 28% L p=0.002 10 0 0 12 24 36 48 Months 87 RENAAL: ARB IS BETTER THAN CONVENTIONAL THERAPY IN TYPE 2 DIABETIC NEPHROPATHY % with Doubling of Baseline Creatinine + ESRD + death 0 Losartan Conventional therapy 25 50 75 100 0 +2– 1 2 4 + 40 – 0– Decrease in Mean Blood Pressure (mm Hg) 3 -2– + 20 – -4– % Reduction 0 – in Proteinuria - 20 – -6– -8– -9– - 10 – -9.2 -9.6 NS p <.001 + 19 - 40 – - 60 – - 45 Brenner et al, N Engl J Med., 2001. 88 THE PROGRAMS OF PREVENTING RENAL DISEASE PROGRESSION WORLDWIDE The funding of such programs is probably on the top of list of the difficulties 89 A GLOBAL FUND TO FIGHT RENAL AND VASCULAR DISEASES ISN: initiator and advisory body in creating the Fund and executing the programs Governed by WHO 90 The notion of health as a good to be bought and sold be cannot be a substitute for the notion of health as a fundamental human right EFFECTS OF LOSARTAN ACCORDING TO THE GEOGRAPHIC AREA: Post-hoc analyses of the RENAAL study Region n° Primary end point p (Doubling s. creat, ESRD or death) Hazard ratio (95 % C.I.) North America 687 0.64 Europe 295 0.76 Latin America 274 0.54 Asia 257 0.0008 Overall (but Asia) 1,256 0.34 Losartan worse Losartan better 0.25 0.5 0.75 1.0 1.25 1.5 The whole effect of Losartan was fully driver by Asian patients 92 1-YEAR PROTEINURIA REDUCTION IN ASIA AND NON-ASIA TYPE 2 DIABETICS ENROLLED IN THE RENAAL STUDY ASIA Non-ASIA n = 257 n = 1,256 Median (I.Q. range) proteinuria reduction vs baseline (%) 0 -5 -10 -9 (-51 to 43) -15 -20 -20 (-55 to 30) p < 0.05 (ANCOVA) Less events in Asia patients were associated with more (double) short-term proteinuria reduction 93 REIN: ACE-I IS MORE CONVENTIONAL THERAPY DISEASE RENOPROTECTIVE THAN IN NON-DIABETIC RENAL 100 % of patients without doubling of baseline creatinine or ESRF Ramipril 80 Conventional therapy 60 P=0.02 40 20 0 0 100 – Diastolic Blood Pressure (mm Hg) 90 – 80 – 70 – 60 – 6 12 18 24 Follow-up 30 36 - 40 – - 20 – % Reduction in Proteinuria 0– 20 – 40 – 60 – Gisen group; Lancet 1997 94 treatment * 100 Glomerular Filtration Rate (ml/min/1.73sqm) 80 60 GFR 20 ml/year GFR 2 ml/year 40 20 DYALISIS 0 -2 -1 0 1 2 3 4 5 years * PA 200/120 mmHg Mogensen et al. , 1976 95 Diabetic nephropathy is irreversible in human No cases of recovery or cure have been reported in the literature Once the clinical signs of nephropathy have become manifest, the natural course is inexorably progressive to death Kussman et al., JAMA, 1976 96 SWIMMING TO REDUCE PROTEINURIA? 20 patients: proteinuric chronic nephropathy Treatments: 12-week regular acquatic exercise Proteinuria Blood pressure p < 0.01 p = 0.005 1.5 150 140 1.0+0.3 120 g / 24h mmHg 130 p < 0.05 1.0 0.5+.03 100 90 80 0.5 70 Pre Post Pre Post Pechter et al., Nephrol Dial Transplant, 200397 … a 22 years old women with previous diagnosis of Systemic Lupus Erythematosus Losartan 50 Renal biopsy * 100 mg/day Hydrochlorotiazide 25 mg/day Low sodium diet 2 g/day Enalapril 2.5 AZA 100 Prednisone 25 10 20 mg/day 5 mg/day MPD 6 2 2 1 0 0 1993 1994 1995 1996 1997 1998 1999 2000 2001 2002 Serum creatinine 3 4 (mg/dl) Proteinuria (g/day) 8 2003 * Severe chronic glomerulopathy with no signs of disease activity 98 PREVENTING MORTALITY? NEPHROPATHY WILL PREVENT CV The BENEDICTstudy ACE-I 1200 type 2 diabetics: BP>140/90 mmHg Normoalbuminuria Main end points: ndCCB Fatal and non-fatal CV events Progression to microalbuminuria Run-in Targets: Study End: ACE-I + ndCCB BP<120/80mhg HbA1c <7,5% Placebo July 2003 0 1 2 3 Years 99 Science brings imagination and vision to bear across the board allowing people to analyze present (and future) situations, make sounder choices, and invest their resources more wisely InterAcademic Council, 2004 On August 30, 2003 World Trade Organization reaches agreement on generic medicines 101 IMPROVING ONLINE ACCESS TO MEDICAL INFORMATION FOR LOW-INCOME COUNTRIES WHO helped to create the Health InterNetwork Access to Research Initiative (HINARI) 69 Low-income countries (GNP<$1,000) offered for free online access to a large library of important international journals 44 Additional countries (GNP $1,000-3,000) qualified for access to the journals at a very low price ($ 1,000 per year) 1043 Total institutions in 100 countries (of a total of 113 eligible countries) have registered for the program 47 Publishers of scientific publishing have joined the Network Access to offer more than 2,300 journals and other full-text resources Aronson, N Engl J Med, 2004 102 Pharmaceutical companies are not the biggest industries in terms of revenues, but are very profitable The pharmaceutical companies average profit is 18 % of revenues as compared to 11.6 % of financial companies Henry and Lexchin, Lancet, 2002 103 The pharmaceutical industry nowadays is a very profitable enterprise, and its returns are on the average greater than those of other industries 104 RESPONSE TO ACE INHIBITION ACCORDING TO DIFFERENT LEVELS OF BASELINE PROTEINURIA 1 .0 ( ml/ min/ mo nt h) Mean rat e of GFR decline 1 .2 Ramipril Convent ional 0 .8 0 .6 0 .4 0 .2 0 n= 1 1 5 n= 6 0 n=81 n=69 <2 2 -3 3 -4 .5 •4 .5 Base-line urinary prot ein excret ion (g/ 2 4 hours) 105