Drugs in Development for

Depression,
Anxiety,
Sleep disorders,
Bipolar Disorder,
Schizophrenia,
and Attention-Deficit Hyperactivity Disorder
(ADHD)
Updated 9/18/2009
*COLOR KEY: ____ - indicates update ____ - indicates discontinued

Depression/Anxiety

Pharmacologic Developmental
Drug Name Company Indication Links
Action Phase
5-HT1A antagonist, Clinical Data Depression, NDA anticipated 1/06 press
Vilazodone
SSRI Online, Inc. Anxiety in late-2009 release
US: Phase III delayed
Valdoxan™ (results not expected
Melatonin agonist, Servier, Depression, Oct ’05 press
(agomelatine, until 2011)
5-HT2B/2C antagonist Novartis Anxiety EU: Approved and release
AGO 178)
launched
5-HT1A partial
Lundbeck, Depression, Phase III delayed
Lu AA21004 agonist, 5-HT3 (results not expected
Takeda Anxiety until 2011)
antagonist
Norepinephrine Depression,
LY2216684 Lilly Phase III
Reuptake Inhibitor ADHD
NE/5-HT reuptake
F2695,
inhibitor, Forest, Pierre Depression,
Levomilnacipran Phase III
enantiomer of Fabre Anxiety
Milnacipran
DA/NE/5-HT Depression,
SEP-227162 Sepracor Phase II
reuptake inhibitor Anxiety
5-HT3, 5-HT2c
antagonism, Lundbeck, Depression, June ’09 press
Lu AA24530 Phase II
reuptake inhibitor Takeda Anxiety release
mechanism?
DA/NE/5-HT Depression,
SEP-225289 Sepracor Phase II
reuptake inhibitor Anxiety
Non-selective
TC-5214 Targacept Depression Phase II
Nicotinic antagonist
Undisclosed Depression,
Lu AA34893 monoamine Lundbeck Bipolar Phase II
modulator Disorder
Losmapimod,
P38 kinase inhibitor GSK Depression Phase II
GSK 856553
Orvepitant, Depression,
NK-1 antagonist GSK Phase II
GW823296 Anxiety
Depression,
AZD6765 NMDA antagonist AstraZeneca Phase II
Anxiety
Ono Depression,
ONO-2333Ms CRF-1 antagonist Phase II
Pharmaceuticals Anxiety
OPC-34712 Otsuka Depression Phase II
Pentapeptide of
Nemifitide (INN melanocyte- [Innapharma’s
Tetragenex Depression Phase II
00835) inhibiting factor info]
(MIF-1)
Depression
SSR 411298 FAAH inhibitor Sanofi-Aventis [in the Phase II
Elderly]
BCI-540 BrainCells, Inc. Depression Phase II
Merck,
ORG 26576 AMPA modulator Depression Phase II
Schering-Plough
TIK-101/D- Tikvah
NMDA antagonist Anxiety, OCD Phase II
Cycloserine Therapeutics
ORG Merck,
GR antagonist Depression Phase II
(34517/34850) Schering-Plough
Depression
GSK561679 GSK [in women Phase II
only]
Tyrima™, Depression,
Reversible MAOI CeNeRx Phase II
CX157 Anxiety
RO4917523,
NMDA antagonist Evotec, Roche Depression Phase II
EVT101
Depression,
GSK 588045 5-HT1 antagonist GSK Phase II
Anxiety
Unknown 5-HT and
RX-10100 Rexahn Depression Phase II
DA modulator
GABA partial
AZD7325 AstraZeneca Anxiety Phase II
agonist
Enkephalinergic
AZD2327 AstraZeneca Anxiety Phase II
modulator
Eisai, M's
SA4503 Sigma agonist Depression Phase II (Europe)
Science
PRE703 MgluR agonist Prescient Anxiety Phase I
JNJ-19567470, Janssen (J & J), Depression, Taisho’s press
CRF-1 antagonist Phase I
TS-041 Taisho Anxiety release
Depression,
SSR 125543 CRF-1 antagonist Sanofi-Aventis Phase I
Anxiety
Undisclosed
SK
YKP3089 mechanism of Anxiety Phase I
Pharmaceuticals
action
Depression,
GSK 163090 5-HT1 antagonist GSK Phase I
Anxiety
Bristol-Myers
GABA-A agonist Anxiety Phase I
Squibb
DA/NE/5-HT Bristol-Myers Depression,
Phase I
reuptake inhibitor Squibb Anxiety
TC-2216 Nicotinic Targacept Depression Phase I
alpha4beta2
 antagonist
Merck, Depression,
URB597 FAAH inhibitor Phase I
Schering-Plough Anxiety
GABA partial
AZD6280 AstraZeneca Anxiety Phase I
agonist
Undisclosed Psylin
PSN0041 Depression Phase I Press release
polypeptide Neurosciences

Sleep disorders
Pharmacologic Developmental
Drug Name Company Indication Links
Action Phase
FDA issued complete
response (9/17/09)
citing benefit-risk
Ciltyri® Sanofi- Sleep [SR 46349 is selective
5-HT2A antagonist problems. Talks
(Eplivanserin) Aventis disorders ongoing for 5-HT2A receptors]
EU decision expected
in Q4’09
5-HT2 antagonist,
Merck, Sleep
ORG 50081 H1 antagonist,
Schering- disorders, hot Phase III
(Esmirtazapine) alpha-adrenergic
Plough flashes
antagonist
Sleep
Tasimelteon, Vanda
Melatonin agonist disorders, Phase III
VEC-162 Pharm.
Depression
Almorexant, GSK, Sleep
Orexin antagonist Phase III
ACT-078573 Actelion disorders
Phase 2 Sleep
PD-6735 Melatonin agonist Phase II
Discovery disorders
Parkinson’s-
Pimavanserin, 5-HT2A inverse Acadia, induced
Phase II 9/2004 Press release
ACP-103 agonist Biovail psychosis,
Sleep
Alpha-2delta
Sleep
PD 200-390 Calcium channel Pfizer Phase II DISCONTINUED
disorders
blocker
GABA-A partial Sleep
EVT 201 Evotec Phase II
agonist disorders
LY2624803, 5-HT2A and H1 Lilly, Sleep
Phase II
HY10275 antagonist Hypnion disorders
Tikvah
TIK-301, Melatonin agonist, Therapeutics, Sleep
Phase II
LY156735 5-HT2B/2C antagonist Phase 2 disorders
Discovery
Sleep
MK4305 Merck Phase II
disorders

Psychosis/Bipolar disorder
Pharmacologic Developmental
Drug Name Company Indication Links
Action Phase
Fanapt® 5-HT2A, D2/D3, and Vanda Pharm. Psychosis APPROVED
 α1 adrenergic
(Iloperidone) (5/6/09)
antagonist
Saphris™
5-HT2 antagonist, Merck, APPROVED
(Asenapine, Psychosis
D2 partial agonist Schering-Plough (8/14/09)
ORG 5222)
5-HT2, 5-HT6, α1 NDA submitted to
Serdolect®
adrenergic, and D2 Lundbeck Psychosis FDA. Approved in
(Sertindole)
antagonist EU.
Bifeprunox (DU- D2/5-HT1A partial Phase III
Solvay, Wyeth Psychosis (resubmission Discontinued
127090) agonist planned for ’09)
Corlux ®, CORT
Psychosis,
108297 Cortisol antagonist Corcept Phase III Corlux info
Depression
(mifespristone)
D2/ D3 partial
Pardoprunox, Psychosis,
agonist, 5-HT1A Solvay Phase III
SLV 308 Parkinson’s
agonist
LIC477D NA+ current Bipolar
Novartis Phase III
(Licarbazepine) blocker disorder
Parkinson’s-
Pimavanserin, 5-HT2A inverse 9/2004 Press
Acadia, Biovail induced Phase III
ACP-103 agonist release
psychosis
ORG Merck, Depression,
GR antagonist Phase II
34517/34850 Schering-Plough Psychosis
Merck,
Psychosis,
ORG 24448 AMPA modulator Schering- Phase II
Depression
Plough, Cortex
Lurasidone D2, 5-HT2A Merck,
Psychosis Phase II
(SM13496) antagonist Sumitomo
RG2417 Bipolar 10/21/05
Prodrug of uridine Repligen Phase II
(triacetyluridine) disorder press release
Lonasen D2, 5-HT2A Dainippon
Psychosis Phase II
(blonanserin) antagonist Pharmaceuticals
R1678 mGluR modulator Roche Psychosis Phase II
LY2140023 mGlu2/3 prodrug Lilly Psychosis Phase II
Mirapex ® Boehringer- Bipolar
D2, D3 agonist Phase II
(pramipexole) Ingelheim disorder
D1/D2 antagonist/5-
LU-31-130 Lundbeck Psychosis Phase II
HT2a antagonist
SM 13496
Sumitomo Psychosis Phase II
(Lurasidone)
Undisclosed Depression,
Lu AA34893 monoaminergic Lundbeck Bipolar Phase II
modulator Disorder
Bipolar
Undisclosed ion
Lu AA39959 Lundbeck Disorder, Phase II
channel modulator
Psychosis
Caripazine, RGH- Forest
D2/D3 antagonist Psychosis Phase II
188 Laboratories
Talnetant (SB- Psychosis,
NK-3 antagonist GSK Phase II
223412) IBS
AVE 1625 CB1 antagonist Sanofi-Aventis Psychosis Phase II
Psychosis,
GW742457 5-HT6 antagonist GSK Phase II
Alzheimer’s
Vabicaserin
5-HT2c agonist Wyeth Depression Phase II
(SCA-136)
Potomac
P-101 Alpha-2 antagonist Phase II
Pharma
Merck,
Org 25935 GLYT1 inhibitor Psychosis Phase II
Schering-Plough
endogenous Psychosis,
RG1068, Secretin pancreatic Repligen Autism, Phase II
hormone Anxiety
ADX63365 MgluR agonist Merck Psychosis Phase II
BL-1020 GABA agonist BioLineRx Psychosis Phase II
TS-032 mGluR modulator Pfizer Psychosis Phase II
PF-217830 Pfizer Psychosis Phase II
PF-2545920 Pfizer Psychosis Phase II
SLV 313 5-HT2A antagonist Solvay Psychosis Phase II
Nicotinic,
ABT-089 Acetylcholine Abbott Psychosis Phase I
agonist
GW773812 D2/5-HT antagonist GSK Psychosis Phase I
SSR 103800 GLYT1 inhibitor Sanofi-Aventis Psychosis Phase I
Alpha/4beta2
Antipsychotic-
nicotinic
TC-1827 Targacept induced side Phase I
acetylcholine
effects
receptor
SK
YKP 1358 Psychosis Phase I
Pharmaceuticals
Johnson &
JNJ-17305600 GLYT1 inhibitor Psychosis Phase I
Johnson
glycine-site specific
XY 2401 Xytis Psychosis Phase I
modulator of NMDA
PNU 170413 Pfizer Psychosis Phase I
RGH-188 D2, D3 antagonist Forrest Psychosis Phase I

Attention Deficit Hyperactivity Disorder (ADHD)

Drug Pharmacologic Developmental
Company Indication Links
Name Action Phase
SPD-465 Long-acting Shire ADHD Approvable, DISCO’D??
(longer amphetamine Pharmaceuticals awaiting final ?
acting product FDA approval
Adderall
XR®)
Intuniv® Alpha-2a- Shire ADHD Approvable,
(SPD503, adrenoceptor Pharmaceuticals expected launch
guanfacine) agonist for late ‘09
Altropane Highly selective DA Boston Life ADHD Phase II
transporter Sciences
radioligand
ABT-089 nicotinic (nAChR) Abbott ADHD Phase II
modulator
ABT-894 nicotinic (nAChR) Abbott ADHD Phase II
modulator
PF- H3 antagonist? Pfizer ADHD Phase II
03654746
Nicotinic alpha7 Memory Memory’s
MEM3454 ADHD Phase II
partial agonist Pharm./ Roche drug profile
Eltroprazine 5-HT1A/1B agonist PsychoGenics ADHD Phase II
DOV-102677 DA/NE/5-HT DOV ADHD, Phase I
reuptake inhibitor Pharmaceuticals Depression
(with preferential
action on the
dopamine
transporter)
SON-216 Sosei ADHD Phase I
(bifemelane)

SPD-483 ATS (Amphetamine Shire ADHD Preclinical

Transdermal Pharmaceuticals
System)

APPENDIX 1

Terms glossary

Phase I:
Phase I includes the initial introduction of an investigational new drug into
humans. Phase I studies are typically closely monitored and may be
conducted in patients or normal volunteer subjects. These studies are
designed to determine the metabolism and pharmacologic actions of the
drug in humans, the side effects associated with increasing doses, and, if
possible, to gain early evidence on effectiveness. During Phase I, sufficient
information about the drug's pharmacokinetics and pharmacological
effects should be obtained to permit the design of well-controlled,
scientifically valid, Phase II studies. The total number of subjects and
patients included in Phase I studies varies with the drug, but is generally
in the range of 20 to 80.

Phase II:
Phase II includes the controlled clinical studies conducted to evaluate the
effectiveness of the drug for a particular indication or indications in
patients with the disease or condition under study and to determine the
common short-term side effects and risks associated with the drug. Phase
II studies are typically well controlled, closely monitored, and conducted in
a relatively small number of patients, usually involving no more than
several hundred subjects.

Phase III:
A phase III trial frequently compares a new treatment to a standard
treatment or to no treatment, and treatment allocation may be randomly
assigned and the data masked. These studies usually involve a large
number of participants followed for longer periods of treatment exposure.
Phase III studies are expanded controlled and uncontrolled trials. Phase
III studies usually include from several hundred to several thousand
subjects.

NDA:
New Drug Application. NDA refers to the data that the drug company
submits to the FDA at the time of the drug’s application filing.

Approvable:
The term given to a drug’s tentative approval status by the FDA. Before
the drug can be launched, the company has to fulfill ongoing clinical and
manufacturing concerns brought up by the FDA.