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Discovering New Therapeutics Uses for Existing Molecules

2012 Industry-Provided Assets

The funding opportunity related to these assets has expired. View the 2014 industry-provided assets.

Assets in this table are alphabetized by mechanism of action. These compounds and biologics have undergone significant pre-clinical and safety testing in humans.

Table of Compounds and Biologics

Code Number & Link to More Information

Mechanism
of Action

Original Development Indication(s)

Route of Administration Formulation Available
(CNS Penetrant+)

AVE5530 (PDF - 128KB)
canosimibe

Acyl-coenzyme A:cholesterol O-acyltransferase (ACAT) inhibitor

Cholesterol absorption inhibitor

Hypercholesterolemia

Oral

SSR149744C (PDF - 145KB)
celivarone

Anti-arrhythmic, Vaughan Williams Class I to IV

Maintenance of sinus rhythm in atrial fibrillation patients

Prevention of shocks and major clinical outcomes in patients with implanted cardiac defibrillator

Oral

PF-05416266 (PDF - 92KB)
senicapoc
(ICA-17043)

Calcium-activated potassium channel blocker (KCa3.1), intermediate-conductance

Sickle cell disease

Asthma

Oral

ABT-639 (PDF - 87KB)

Calcium channel, voltage-gated (Cav3.2, T-type) blocker

Pain

Oral
(Yes)

CP-945598 (PDF - 126KB)
otenabant

Cannabinoid receptor 1 (CB1) antagonist

Obesity

Oral
(Yes)

LY2828360 (PDF - 92KB)

Cannabinoid receptor 2 (CB2) agonist

Osteoarthritis pain

Oral
(Yes)

AZD1981 (PDF - 115KB)

Chemoattractant receptor-homologous molecule expressed on Th2 cells (CRTh2)/prostaglandin D2 (DP2) receptor antagonist

Asthma

Chronic obstructive pulmonary disease

Oral

SSR150106 (PDF - 151KB)

Chemokine receptor antagonist (TNFα release)

Rheumatoid arthritis pain

Oral

AZD2423 (PDF - 96KB)

Chemokine (C-C motif) receptor 2 (CCR2) antagonist

Chronic obstructive pulmonary disease

Pain

Oral

PF-04136309 (PDF - 169KB)

Chemokine (C-C motif) receptor 2 (CCR2) antagonist

Chronic osteoarthritis pain

Oral
(No)

CE-326597 (PDF - 152KB)

Cholecystokinin 1 receptor (CCK-1R) (or CCKA receptor) agonist

Obesity in type II diabetes

Oral

BMS-562086 (PDF - 89KB)
pexacerfont

Corticotropin-releasing factor 1 (CRF1) receptor antagonist

Major depressive disorder

Generalized anxiety disorder

Irritable bowel syndrome

Oral
(Yes)

JNJ-39269646 (PDF - 94KB)

Fast dissociating D2/D3/5-HT6 antagonist

Schizophrenia

Oral
(Yes)

ZD4054 (PDF - 92KB)
zibotentan

Endothelin receptor A (ETA) antagonist

Oncology

Pulmonary artery hypertension

Oral

PF-00913086 (PDF - 200KB)
prinaberel
(ERB-041)

Estrogen receptor β (ERβ, ESR2) agonist/nuclear receptor 3A2 (NR3A2) agonist

Endometriosis

Oral

LY500307 (PDF - 101KB)

Estrogen receptor β (ERβ, ESR2) agonist/nuclear receptor 3A2 (NR3A2) agonist

Benign prostatic hyperplasia

Lower urinary tract symptoms

Oral

XRP0038 (PDF - 200KB)
Riferminogene pecaplasmid, NV1FGF, temusi

Non-viral fibroblast growth factor 1 (NV1FGF)

Critical limb ischemia

Intramuscular
(No)

AZD7325 (PDF - 153KB)

γ-Aminobutyric acid (GABA) A receptor, alpha 2 (GABAA α2) agonist

Generalized anxiety disorder

Oral
(Yes)

AZD3355 (PDF - 167KB)
lesogaberan

γ-Aminobutyric acid (GABA) B receptor, 1 (GABAB1) agonist

Gastroesophageal reflux disease

Oral

PF-05190457 (PDF - 77KB)

Ghrelin receptor (growth hormone secretagogue 1a receptor, GHS-1aR) inverse agonist, competitive antagonist

Type II diabetes

Oral
(Yes)

AZD1656 (PDF - 1656KB)

Glucokinase (GK) activator

Diabetes

Oral

BMS-820132 (PDF - 82KB)

Glucokinase (GK) activator

Type II diabetes

Oral

PF-03463275 (PDF - 138KB)

Glycine transporter 1 (GlyT1) inhibitor

Solute carrier family 6 (neurotransmitter transporter, glycine), member 9 (SLC6A9) inhibitor

Schizophrenia

Oral
(Yes)

HMR1766 (PDF - 122KB)
ataciguat

Soluble guanylate cyclase (sGC) activator

Angina pectoris

Peripheral artery disease

Neuropathic pain

Oral

GSK1004723 (PDF - 116KB)

Histamine H1/H3 receptor antagonist

Allergic rhinitis

Topical
(No)

GSK835726 (PDF - 109KB)

Histamine H1/H3 receptor antagonist

Allergic rhinitis

Oral
(No)

ABT-288 (PDF - 78KB)

Histamine H3 receptor antagonist

Cognition
(cognitive deficits of schizophrenia)

Oral
(Yes)

PF-03654746 (PDF - 192KB)

Histamine H3 receptor antagonist

Narcolepsy

Cognition

Attention deficit hyperactivity disorder

Allergic rhinitis

Oral
(Yes)

CE-210666 (PDF - 113KB)

5-Hydroxytryptamine 1B receptor (5-HT1B) antagonist

Depression

Oral
(Yes)

CP-448187 (PDF - 142KB)
elzasonan

5-Hydroxytryptamine 1B receptor (5-HT1B) antagonist

Depression

Oral
(Yes)

PH-670187 (PDF - 123KB)
dermaciclane, EGIS-3886

5-Hydroxytryptamine 2A/2C receptor (5-HT2A/2C) antagonist

Generalized anxiety disorder

Oral
(Yes)

PF-04995274 (PDF - 138KB)

5-Hydroxytryptamine 4 receptor (5-HT4) partial agonist

Gastroesophageal reflux disease

Alzheimer's disease

Oral
(Yes)

JNJ-18038683 (PDF - 67KB)

5-Hydroxytryptamine 7 receptor (5-HT7) antagonist

Major depressive disorder

Oral
(Yes)

LY2590443 (PDF - 70KB)

5-Hydroxytryptamine 7A receptor (5-HT7A) antagonist

Migraine

Oral

MEDI2338 (PDF - 105KB)

Interleukin-18 (IL-18) inhibitor

Chronic obstructive pulmonary disease

Coronary heart disease

Intravenous, subcutaneous

PF-04191834 (PDF - 130KB)

5-Lipoxygenase (5-LO) inhibitor

Asthma

Chronic osteoarthritis pain

Oral
(Yes)

SD-7300 (PDF - 137KB)
(SC-81490)

Matrix metalloproteinase 2, 9, and 13 (MMP-2, -9, -13) inhibitor

Post-myocardial infarction cardiac remodeling

Disease-modifying osteoarthritis drug

Oral

AZD1236 (PDF - 78KB)

Matrix metalloproteinase 9|12 (MMP9|MMP12) inhibitor

Chronic obstructive pulmonary disease

Oral

BMS-830216 (PDF - 79KB)

Melanin-concentrating hormone 1 (MCH1) receptor antagonist

Obesity

Oral
(Yes)

AZD5904 (PDF - 93KB)

Myeloperoxidase (MPO) inhibitor

Chronic obstructive pulmonary disease

Multiple sclerosis

Oral

SAR103168 (PDF - 145KB)

Multi-kinase inhibitor

Liquid tumors (acute myeloid leukemia)

Intravenous

ABT-089 (PDF - 107KB)

Nicotinic acetylcholine receptor (nAChR) partial agonist (α4β2* subtypes)

Alzheimer's disease

Attention deficit hyperactivity disorder

Oral
(Yes)

CP-601927 (PDF - 182KB)

Nicotinic acetylcholine receptor α4β2 (α4β2 nAChR) partial agonist

Multiple CNS

Oral
(Yes)

AZD0328 (PDF - 94KB)

Nicotinic acetylcholine receptor alpha 7 (α7 nAChR) agonist

Cognitive impairment

Oral
(Yes)

JNJ-39393406 (PDF - 118KB)

Nicotinic acetylcholine receptor, α7 (α7nAChR) positive allosteric modulator

Cognitive impairment in schizophrenia

Oral
(Yes)

GW274150 (PDF - 110KB)

Inducible nitric oxide synthase (iNOS) inhibitor

Migraine (acute and prophylaxis)

Asthma

Rheumatoid arthritis

Sepsis

Oral
(Poor)

SD-6010 (PDF - 83KB)
(SC-84250)

Inducible nitric oxide synthase (iNOS) inhibitor

Asthma

Osteoarthritis pain

Disease-modifying osteoarthritis drug

Oral

AZD7268 (PDF - 193KB)

δ Opioid receptor agonist

Anxiety

Depression

Oral
(Yes)

AVE8134 (PDF - 117KB)

Peroxisome proliferator-activated receptor α (PPARα)/nuclear receptor 1C1 (NR1C1) agonist

Type II diabetes

Oral

AVE0847 (PDF - 189KB)

Peroxisome proliferator-activated receptor α/γ (PPARα/γ)/nuclear receptor 1C1/1C3 (NR1C1/1C3) agonist

Type II diabetes

Oral

PF-05019702 (PDF - 139KB)
(PRA-27)

Progesterone receptor (PR) antagonist/nuclear receptor 3C3C (NRC3C) antagonist

Endometriosis

Oral

AZD9056 (PDF - 115KB)

Purinergic receptor 2X, ligand-gated ion channel, 7 (P2X7) antagonist

Chronic obstructive pulmonary disease

Crohn's disease

Osteoarthritis

Rheumatoid arthritis

Oral

LY2245461 (PDF - 71KB)

Selective estrogen receptor modulator (SERM)

Hot flashes in postmenopausal women

Oral

AZD0530 (PDF - 65KB)
saracatinib

Src tyrosine kinase inhibitor

Oncology

Oral

SB223412 (PDF - 122KB)
talnetant

Tachykinin receptor/neurokinin 3 (NK3) receptor antagonist

Cough

Chronic obstructive pulmonary disease

Schizophrenia

Irritable bowel syndrome

Overactive bladder

Oral
(Yes)

SAR115740 (PDF - 146KB)

Transient receptor potential cation channel vanilloid 1 (TRPV1) antagonist

Acute and chronic pain

Oral

SSR97225 (PDF - 150KB)

β-Tubulin-binding agent with dual mechanism

Solid tumor

Intravenous, injectable suspension

AZD2171 (PDF - 123KB)
cediranib

Vascular endothelial growth factor receptor (VEGFR) 1, 2, and 3 tyrosine kinase inhibitor

Oncology

Oral

+CNS penetrant: Yes, no or unknown.

Last updated: 08-15-2017
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