R&D Pipeline (November 2005) 1Japan (1)Filed Code No YM905 YM177 YM152 FK463 Generic Name (Filing Date ) solifenacin (Aug 2004) celecoxib (Dec 2002) finasteride (Dec1994) micafungin (July 2004) (Oct 2005) Therapeutic Target Urinary frequency, urinary incontinence or urgency associated with overactive bladder Rheumatoid arthritis, osteoarthritis, low back pain, etc Classification Muscarinic receptor antagonist In-house Cyclooxygenase-II inhibitor Pfizer Benign prostatic hyperplasia 5 alpha-reductase inhibitor Merck Deep-seated fungal infection (for pediatric) Candin antifungal agent Injection In-house Lupus nephritis Immunosuppressant In-house (2)Preparation for Filing YM060 ramosetron Irritable bowel syndrome (IBS) 5HT 3 antagonist In-house (3)Phase-III YM529 minodronate Osteoporosis Bisphosphonate In-house YM617 tamsulosin Lower urinary tract syndrome Alpha-1 receptor antagonist In-house YM086 telmisartan Diabetic nephropathy YM643 interferon alfacon-1 Chronic hepatitis C virus infection (advaferon for use in combination with ribavirin) Angiotensin II receptor antagonist Consensus interferon (CIFN) Injection/ ribavirin: Boehringer Ingelheim Schering- Plough
YM026 YM026 YM177 nateglinide nateglinide celecoxib Type II diabetes (concomitant treatment with biganides) Type II diabetes (concomitant treatment with insulin sensitizers) Post surgical pain, post traumatic pain, tooth extract pain Rapid onset insulin secretion enhancer Rapid onset insulin secretion enhancer Ajinomoto Ajinomoto Cyclooxygenase-II inhibitor Pfizer Ulcerative colitis Immunosuppressant In-house YM1170 telithromycin Pediatric use Ketolide class antibiotic famotidine Symptomatic-gastro-esophageal reflux disease(s-gerd) H 2 receptor antagonist In-house Myasthenia gravis (all) Immunosuppressant In-house FK199B(*) zolpidem Insomnia (modified release) Omega-1 receptor agonist * FK199B:In preparation for P-III studies (4)Phase-II YM974 valdecoxib Rheumatoid arthritis, osteoarthritis, low back pain, etc Cyclooxygenase-II inhibitor Pfizer YM978 parecoxib Acute pain Cyclooxygenase-II inhibitor Injection Pfizer FK949 quetiapine fumarate Behavior psychological symptoms of dementia FK481 strontium ranelate Osteoporosis YM533 beraprost Suppression of organ rejection in organ transplant (modified release) Chronic renal failure (primary / nephrosclerosis) Antipsychotic AstraZeneca Bone formation stimulating and antiresorptive agent Servier Immunosuppressant In-house Prostacyclin receptor stimulator Toray
2USA (1)Filed Code No Generic Name Therapeutic Target Classification (Product Name) (Filing Date) conivaptan YM087 Hyponatremia Vasopressin receptor antagonist Injection In-house (Jan2004) * Received approvable letter from FDA in November, 2004 (2)Preparation for Filing Suppression of organ rejection in organ transplant (modified release) Immunosuppressant In-house RSD1235 Atrial fibrillation and atrial flutter Antiarrhythmic agent Injection Cardiome (3)Phase-III Rheumatoid arthritis Immunosuppressant In-house Atopic dermatitis Immunosuppressant Cream In-house CVT-3146 regadenoson Pharmacologic stress agent in cardiac perfusion imaging studies Adenosine A 2 a agonist Injection CV Therapeutics Psoriasis Immunosuppressant Cream In-house
(4)Phase-II YM443 Functional dyspepsia Acetylcholine level enhancer Zeria FK778 carperitide Suppression of organ rejection in liver and kidney transplants Acute heart failure Immunosuppressant Alfa-human atrial natriuretic peptide Injection Daiichi Asbio FK962 Alzheimer s disease Antidementia In-house YM155 Hormone refractory prostate cancer, Non small cell lung cancer, Metastatic melanoma, etc Survivin expression inhibitor Injection In-house Asthma Immunosuppressant Inhalation In-house 3Europe (1)Preparation for Filing FK463 micafungin Deep-seated fungal infection Candin antifungal agent Injection In-house Suppression of organ rejection in organ transplant (modified release) Immunosuppressant In-house
(2)Phase-II YM178 YM150 Urinary frequency, urinary incontinence or urgency associated with overactive bladder Prevention of venous thromboembolism (VTE) after major orthopedic surgery, Prophylaxis of thromboembolic complications associated with atrial fibrillation(af) Beta 3 receptor agonist In-house Factor Xa inhibitor In-house YM060 ramosetron Irritable bowel syndrome (IBS) 5HT 3 antagonist In-house YM617 tamsulosin Functional symptoms with benign prostatic hyperplasia Alpha-1 receptor antagonist In-house ly disintegrating tablet Rheumatoid arthritis Immunosuppressant In-house FK778 Suppression of organ rejection in liver and kidney transplants Immunosuppressant Asthma Immunosuppressant Inhalation In-house YM155 Hormone refractory prostate cancer, Non small cell lung cancer, Metastatic melanoma, etc Survivin expression inhibitor Injection In-house 4Projects at Early Stage (Phase-I/Pre-clinical): 23 5Project Discontinued Code No(Generic Name) Stage Therapeutic Target Reason telithromycin Filed (Japan) Skin and soft tissue infections & cervicitis FK614 P-II (Japan/USA) Non-insulin dependent diabetes mellitus (NIDDM) - withdrew the filing for these indications since efficacy of telithromycin couldn t be expected superior to those of existing agents Efficacy and safety profile of FK614 were considered to be similar to those of existing PPAR agonists, and no remarkable advantages over competitors could not be observed
Changes from the previous announcement (R&D Meeting in July 2005) - snda of LUVOX (fluvoxamine maleate) for the treatment of social anxiety disorder was approved in Japan on October 11, 2005 - snda of telithromycin for the treatment of skin and soft tissue infections & cervicitis was withdrawn in Japan - snda of for the treatment of lupus nephritis was filed in Japan on October 12, 2005 - Development status of YM060 for the treatment of Irritable bowel syndrome (IBS) progressed from Phase-III to the preparation for NDA in Japan - Development status of Myslee modified release (FK199B) for the treatment of Insomnia is in preparation for P-III studies in Japan - Phase-III of for the treatment of myasthenia gravis was initiated in Japan - Phase-II of FK614 for the treatment of non-insulin dependent diabetes mellitus was terminated in Japan and the US - Phase-II of YM533 for the treatment of chronic renal failure (primary/nephrosclerosis) was initiated in Japan - Development status of modified release for the treatment of suppression of organ rejection in organ transplant progressed from Phase-III to the preparation for NDA in the US and MAA in Europe - Development status of RSD1235 for the treatment of atrial fibrillation and atrial flutter progressed from Phase-III to the preparation for NDA in the US