Presentation of March 2011
Financial Results
Status of R&D Pipeline〇Progress in fiscal 2010 and initiatives in fiscal 2011

Director, KYORIN Co., Ltd.
KYORIN Pharmaceutical CoCo., Ltd.
Ltd
Representative Director,
President and Chief Executive Officer
K iji Hirai
Keiji
Hi i0

Aim for Early Launch of Newly Developed Products andEnhance and Strengthen the Pipeline

Tasks atEach Stage

HOPE 100 Stage 1
FY2010-2015

HOPE 100 Stage 2
FY2016-2019

HOPE 100 Stage 3
FY2020-2023

・LCM promotion
・KRP-108 (aim for FY2014 launch)
・KRP-104 (aim to out-license)

Early application and approvalof newly developed products
Pipeline enhancement andstrengthening

Create original new
global products

Aim to in-license products

LCM
Newly DevelopedProducts
Incl. products
Inclprod cts
in-licensed

Drugs
Originated
In-House

Mucodyne DS50 Uritos OD tablet
New usages and dosages (QD) for Pentasa, newdrug formulations (suppositories)
KRP-108 (asthma)
KRP-104 (diabetes)
Candidates for in-licensing(respiratory ,otolaryngology and urology)
In-licensing of aclidinium (Feb. 2011)

LCM: Life Cycle Management
AS-3201 (diabetic neuropathy)
KRP-209 (tinnitus)
KRP-203 (immunomodulator: IBD)KRP 110 (constipation and intractable pruritus)
KRP-110
KRP-A B 1102 (COPD)
KRP-AM1977X (respiratory infection)
KRP-AM1977Y (anti-MRSA)

Priority Fields for In-House
In House Drugs: Respiratory
Respiratory, Urological
Urological, Infections
Infections, Others■Clarify direction of R&D (Concentrate on FC domain and respond to unmet medical needs)・Strengthen R&D portfolio management (development pipeline)
・Evaluation and swift decisions on development projects (early development projects: incl. PCC, POC)
■Strengthen capacity to create new drugs (restructure the drug discovery network)
・Review ActivX and KSRL functions (Drug discovery bases in priority domains: cancer research,respiratory research)
・Proactive external collaboration (academia, others)

1Drug Development Pipeline: Progress in FY2010((In-House)
)
～PhⅠ

PhⅡ

KRP-AB1102
Respiratory

PhⅢ
KRP-108
KRP
108

PreparingPi
forfclinical trials

Ph III from August

Approval/Launch

Mucodyne
DS50%
On market in May

Uritos OD
tablets

UrologicalOn market in April
2011

Otolaryngol
ogicalKRP-209

Infections

KRP-AM1977

Mucodyne
DS50%
On market in May

Ph I preparationsPentasa (UC)once a day
Pentasa (UC)suppository

KRP-203
Ph I Japanese subjects
Start in December

OtherApplication

KRP-110

KRP-104

Ph I from August(Overseas)

Ph IIb completed(overseas)

AS-3201
Ph IIb completed

Information in the dotted red box are changes sincetthee aannouncement
ou ce e t ofo fiscal
sca 2010
0 0 tthird-quarterd qua tefinancial results
Items in red are changes since the announcement offinancial results for fiscal 20092COPD Treatment Agent: KRP-AB1102
Action: Long-acting muscarine M3 antagonist (LAMA)
A ti iingredient
Activedi t: Aclidinium Bromide
Formulation: Dry Powder Inhaler
Features：z Fewer sistemic side effectsz Twice-daily dosage improves symptoms and respiratory function
throughout a day
z Short period reaching maximum effectz Easy-to-use inhaler device

Dry powder inhaler: Genuair®
3

Antibacterial agent: KRP-AM1977
Next-generation quinolone antibacterial agent (anti-MRSA,respiratory) developed by KYORIN Pharmaceutical〔F t〔Features〕〕
z Superior ability to over come drug-resistant gram-positive bacteria (incl. MRSA)z Outstanding ADME comparable to GFLX (oral absorption, tissue penetration)z Higher safety margin is expected by results of preclinical studies
Cumulative %KRP-AM1977Y¾Planning¾Pli development
dlt off aninjection as an anti-MRSA drug

Cumulative %PCG low-sensitivity pneumococcus

KRP-AM1977X¾ Planning development as an oral
treatment for respiratory infection(including otolaryngology)

4

Drug Development Pipeline: Progress in FY2010((In-House)
)
～PhⅠ

PhⅡ

KRP-AB1102
Respirator
Respiratory

PhⅢ

Application

Approval/Launch

KRP-108(COPD)
Entering clinical
trials(Asthma)

UrologicalOtolaryngol
ogicalKRP-209

KRP-209((Tinnitus))

KRP-AM1977
Infections(Antibacterial agent)Enteringg Ph I

KRP-203
KRP-110
Other

Opioid-induced
constipation treatment(overseas)

KRP-203(IBD)

KRP-104(diabetes)

Pentasa (UC)suppository
Pentasa (UC)once a day

Pentasa (UC)once a day

Aim toout-license

AS-3201
AS3201(Diabeticneuropathy)

5

Main R&D Activities① （ May 11 , 2011 Release)※：Changes since previous announcement

Ph IIb Application submitted
Stage(3Q of fiscal 2010) shown

Compound/C d/CodeTherapy
area/Action/A ti

OriginPhⅢ(12/2009)

Pentasa(tablet)

Ulcerativecolitis

FerringPharmaceuticals

New dosage regimen for ulcerative colitis in theremission phase (once a day)PhⅢ
(11/2010)

Pentasa(suppository)

Ulcerativecolitis

FerringPharmaceuticals

Consideration of a new dosage form for the active
phase of ulcerative colitis(once a day)*Development of a newdosage form

Japan

OverseasFeatures

Comments

PhⅢ(8/2010)(US)
SkyePharma: Applicationppsubmitted (3/2009)（Europe）
Mundipharma: Application
submitted (3/2010)

KRP-108(Inhaleddrug)

Antiasthmatic

SkyePharma PLC

An ICS/LABA combination product, which offers
better compliance and convenience to the patients・License agreement with
SkyePharma (4/2008)
・Ph II completed indomestic (4/2010)

PhⅡ(3/2005)

Eisai: Ph III

AS-3201(tablet)Diabetic
neuropathy

Dainippon
Sumitomo

Aldose reductase inhibitor to reduce the sorbitol
accumulation in the cell, and improve diabetic
neuropathy

・Co-development with
Dainippon Sumitomo(domestic only)
・Ph II completed indomestic (3/2011) ※PhⅡ（2/2008）

PhⅡ（9/2007）

KRP-104

Antidiabetes
agent

In-house

A DPPIV inhibitor to reduce blood glucose
through suppression of the degradation ofinsulin-releasing hormone. Diabetic therapy withfewer side effects is expected than existingtreatments.

・Ph II b in overseas(11/2009)
・Ph II b in domestic
completed (3/2010)

Oth Comments
OtherCt
・Uritos OD Tablet 0.1mg (orally disintegrating tablet of immidafenasin (INN), a drug for overactive bladder:Application (4/2011) ※6

Main R&D Activities② （ May 11 , 2011 Release)※：Changes since previous announcement

POC Project (Pre-clinical ~ Ph II)
StageJapanOverseas

Compound/CodeTherapy
area/Action(3Q of fiscal 2010) shown
OriginFeatures

Comments

ＰｈⅠ
preparations

KRP-AM1977X ※(Oral agent）

New quinolone
synthetic
antibacterial agent

In-house

ＰｈⅠ
preparations

KRP-AM1977Y ※(Injection）

New quinolone
synthetic
antibacterial
tib t i l agentt

In-house（Europe）
Almirall: Preparing
for application((US))
ForestPharmaceuticals: Preparing
for application※KRP-AB1102（Inhaled drug）

Chronic
Obstructive
Pulmonary Disease(COPD)

AlmirallThis bronchodilating agent has an acetylcholine
receptor antagonist action that offers long-lasting
improvement for breathing difficulty and shortnessof breath associated with COPD.
①Fewer sistemic side effects①②Twice-daily dosage improves symptoms andrespiratory function throughout a day③Short period reaching maximum effect

PhⅠ（8/2010）

KRP 110
KRP-110

Opioid-induced
Opioidinducedconstipation andintractable pruritus

In house
In-house

A highly selective μμ-opioid
opioid receptor antagonist.
antagonist It isexpected to block constipation induced by opioid
analgesics without interrupting the analgesic effectof opioids. It is orally effective in various itchingmodels, indicating potential of a novel anti-itch drugfor intractable pruritus.

PhⅠ（12/2010）

PhⅡ（POC)(12/2010)(Novartis)

KRP-203

Transplantation
and autoimmune
diseases treatment
IBD

In-house

An immunosuppressant with a novel mechanism
called an S1P-agonist. It may have a better safety
profile than previous ones as well as an excellent
effect under concomitant use with other types ofimmunomodulator.

License agreement with
Novartis (2/2006)
New license agreement
IBD (11/2010)

ＰｈⅡ
preparations

PhⅢ
Merz

KRP-209

Tinnitus

Merz

KRP-209 (Neramexane) is expected to improve thepatients' annoyance and difficulties in their life
caused by tinnitus mainly through its two
pharmacological properties: 1) NMDA antagonistic
activity and 2) Nicotinic acetylcholine antagonistic
activity

License agreement withMerz (11/2009)
Ph I clinical trial in
Japanese (single dosePK) in US completed byMerz (3/2010)

Preparingfor clinical
trials①Superior ability to combat drug-resistant grampositive bacteria (incl. MRSA)②Outstanding ADME (oral absorption, tissue
migration)③High degree of safety expected since safety
prior to clinical trials
hurdles cleared pLicense agreement withAlmirall (2/2011)

7

Main R&D Activities③ （ May 11 , 2011 Release)※：Changes since previous announcement

Licensing Development
Compound/CodeLicensee/Collaborativeresearch(3Q of fiscal 2010) shown
Stage

Alphagan/AlphaganP

Senju Seiyaku

Application
submitted（3/2011）

Ketas

MediciNova (US)KCA-757
KCA
757

KRP-203

Therapy area/Action

OriginComments

Glaucoma

Allergan (US)・Licensed from Allergan(Cross license of gatifloxacin ophthalmic solution)
・License-out to Senju (5/2004)

Overseas Ph II（（8/2005））

Cerebrovasculardisorders

In-house・KYORIN grants MediciNova an exclusive license in
p for Japan,p , China,,
all countries worldwide except
South Korea and Taiwan to develop, manufactureand sell the compound and products for the multiple
sclerosis indication (10/2004)
Result of Ph II was reported in April 2008

MediciNova (US)Overseas Ph III(Anti-bronchial
Asthma: 11/2006)
Overseas PhⅡ/Ⅲ(Interstitial cystitis:5/2005)

Anti bronchial asthma
Anti-bronchialand interstitial cystitis
agent

In-house
Inhouse・KYORINKYORIN grants MediciNova an exclusive license in
all countries worldwide except for Japan, China,
South Korea and Taiwan to develop and sell thecompound and products・Interstitial cystitis: Result of Ph II/III was reported inpceased
Januaryy 2007 and development
・Bronchial asthma: Clinical trial overseas wasdiscontinued.

Novartis (Switzerland)Overseas PhⅡ（POC)（12/2010）

Transplantation andautoimmune diseases
IBD*In-house

・Granted right to develop and commercialize KRP-203
worldwide for use as an
immunosuppressant in organ transplants, and right todevelop and commercialize KRP-203 worldwide
except in Japan, Korea,
China and Taiwan for the treatment of autoimmunediseases and other diseases (February 2006)）*New license agreement IBD (November 2010※8