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Research

2012 Industry-Provided Agents

medicines

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

These compounds and biologics have undergone significant pre-clinical and safety testing in humans.

Table of Compounds and Biologics*

Code Number & Link to More InformationMechanism
of Action
Original Development Indication(s)Route of Administration Formulation Available
(CNS Penetrant+)
AVE5530
canosimibe
Acyl-coenzyme A:cholesterol O-acyltransferase (ACAT) inhibitor

Cholesterol absorption inhibitor
HypercholesterolemiaOral
SSR149744C
celivarone
Anti-arrhythmic, Vaughan Williams Class I to IVMaintenance of sinus rhythm in atrial fibrillation patients

Prevention of shocks and major clinical outcomes in patients with implanted cardiac defibrillator
Oral
PF-05416266
senicapoc
(ICA-17043)
Calcium-activated potassium channel blocker (KCa3.1), intermediate-conductanceSickle cell disease

Asthma
Oral
ABT-639Calcium channel, voltage-gated (Cav3.2, T-type) blockerPainOral
(Yes)
CP-945598
otenabant
Cannabinoid receptor 1 (CB1) antagonistObesityOral
(Yes)
LY2828360Cannabinoid receptor 2 (CB2) agonistOsteoarthritis painOral
(Yes)
AZD1981Chemoattractant receptor-homologous molecule expressed on Th2 cells (CRTh2)/prostaglandin D2 (DP2) receptor antagonistAsthma

Chronic obstructive pulmonary disease
Oral
SSR150106Chemokine receptor antagonist (TNFα release)Rheumatoid arthritis painOral
AZD2423Chemokine (C-C motif) receptor 2 (CCR2) antagonistChronic obstructive pulmonary disease

Pain
Oral
PF-04136309Chemokine (C-C motif) receptor 2 (CCR2) antagonistChronic osteoarthritis painOral
(No)
CE-326597Cholecystokinin 1 receptor (CCK-1R) (or CCKA receptor) agonistObesity in type II diabetesOral
BMS-562086
pexacerfont
Corticotropin-releasing factor 1 (CRF1) receptor antagonistMajor depressive disorder

Generalized anxiety disorder

Irritable bowel syndrome
Oral
(Yes)
JNJ-39269646Fast dissociating D2/D3/5-HT6 antagonistSchizophreniaOral
(Yes)
ZD4054
zibotentan
Endothelin receptor A (ETA) antagonistOncology

Pulmonary artery hypertension
Oral
PF-00913086
prinaberel
(ERB-041)
Estrogen receptor β (ERβ, ESR2) agonist/nuclear receptor 3A2 (NR3A2) agonistEndometriosisOral
LY500307Estrogen receptor β (ERβ, ESR2) agonist/nuclear receptor 3A2 (NR3A2) agonistBenign prostatic hyperplasia

Lower urinary tract symptoms
Oral
XRP0038
Riferminogene pecaplasmid, NV1FGF, temusi
Non-viral fibroblast growth factor 1 (NV1FGF)Critical limb ischemiaIntramuscular
(No)
AZD7325γ-Aminobutyric acid (GABA) A receptor, alpha 2 (GABAA α2) agonistGeneralized anxiety disorderOral
(Yes)
AZD3355
lesogaberan
γ-Aminobutyric acid (GABA) B receptor, 1 (GABAB1) agonistGastroesophageal reflux diseaseOral
PF-05190457Ghrelin receptor (growth hormone secretagogue 1a receptor, GHS-1aR) inverse agonist, competitive antagonistType II diabetesOral
(Yes)
AZD1656Glucokinase (GK) activatorDiabetesOral
BMS-820132Glucokinase (GK) activatorType II diabetesOral
PF-03463275Glycine transporter 1 (GlyT1) inhibitor

Solute carrier family 6 (neurotransmitter transporter, glycine), member 9 (SLC6A9) inhibitor
SchizophreniaOral
(Yes)
HMR1766
ataciguat
Soluble guanylate cyclase (sGC) activatorAngina pectoris

Peripheral artery disease

Neuropathic pain
Oral
GSK1004723Histamine H1/H3 receptor antagonistAllergic rhinitisTopical
(No)
GSK835726Histamine H1/H3 receptor antagonistAllergic rhinitisOral
(No)
ABT-288Histamine H3 receptor antagonistCognition
(cognitive deficits of schizophrenia)
Oral
(Yes)
PF-03654746Histamine H3 receptor antagonistNarcolepsy

Cognition

Attention deficit hyperactivity disorder

Allergic rhinitis
Oral
(Yes)
CE-2106665-Hydroxytryptamine 1B receptor (5-HT1B) antagonistDepressionOral
(Yes)
CP-448187
elzasonan
5-Hydroxytryptamine 1B receptor (5-HT1B) antagonistDepressionOral
(Yes)
PH-670187
dermaciclane, EGIS-3886
5-Hydroxytryptamine 2A/2C receptor (5-HT2A/2C) antagonistGeneralized anxiety disorderOral
(Yes)
PF-049952745-Hydroxytryptamine 4 receptor (5-HT4) partial agonistGastroesophageal reflux disease

Alzheimer's disease
Oral
(Yes)
JNJ-180386835-Hydroxytryptamine 7 receptor (5-HT7) antagonistMajor depressive disorderOral
(Yes)
LY25904435-Hydroxytryptamine 7A receptor (5-HT7A) antagonistMigraineOral
MEDI2338Interleukin-18 (IL-18) inhibitorChronic obstructive pulmonary disease

Coronary heart disease
Intravenous, subcutaneous
PF-041918345-Lipoxygenase (5-LO) inhibitorAsthma

Chronic osteoarthritis pain
Oral
(Yes)
SD-7300
(SC-81490)
Matrix metalloproteinase 2, 9, and 13 (MMP-2, -9, -13) inhibitorPost-myocardial infarction cardiac remodeling

Disease-modifying osteoarthritis drug
Oral
AZD1236Matrix metalloproteinase 9|12 (MMP9|MMP12) inhibitorChronic obstructive pulmonary diseaseOral
BMS-830216Melanin-concentrating hormone 1 (MCH1) receptor antagonistObesityOral
(Yes)
AZD5904Myeloperoxidase (MPO) inhibitorChronic obstructive pulmonary disease

Multiple sclerosis
Oral
SAR103168Multi-kinase inhibitorLiquid tumors (acute myeloid leukemia)Intravenous
ABT-089Nicotinic acetylcholine receptor (nAChR) partial agonist (α4β2* subtypes)Alzheimer's disease

Attention deficit hyperactivity disorder
Oral
(Yes)
CP-601927Nicotinic acetylcholine receptor α4β2 (α4β2 nAChR) partial agonistMultiple CNSOral
(Yes)
AZD0328Nicotinic acetylcholine receptor alpha 7 (α7 nAChR) agonistCognitive impairmentOral
(Yes)
JNJ-39393406Nicotinic acetylcholine receptor, α7 (α7nAChR) positive allosteric modulatorCognitive impairment in schizophreniaOral
(Yes)
GW274150Inducible nitric oxide synthase (iNOS) inhibitorMigraine (acute and prophylaxis)

Asthma

Rheumatoid arthritis

Sepsis
Oral
(Poor)
SD-6010
(SC-84250)
Inducible nitric oxide synthase (iNOS) inhibitorAsthma

Osteoarthritis pain

Disease-modifying osteoarthritis drug
Oral
AZD7268δ Opioid receptor agonistAnxiety

Depression
Oral
(Yes)
AVE8134Peroxisome proliferator-activated receptor α (PPARα)/nuclear receptor 1C1 (NR1C1) agonistType II diabetesOral
AVE0847Peroxisome proliferator-activated receptor α/γ (PPARα/γ)/nuclear receptor 1C1/1C3 (NR1C1/1C3) agonistType II diabetesOral
PF-05019702
(PRA-27)
Progesterone receptor (PR) antagonist/nuclear receptor 3C3C (NRC3C) antagonistEndometriosisOral
AZD9056Purinergic receptor 2X, ligand-gated ion channel, 7 (P2X7) antagonistChronic obstructive pulmonary disease

Crohn’s disease

Osteoarthritis

Rheumatoid arthritis
Oral
LY2245461Selective estrogen receptor modulator (SERM)Hot flashes in postmenopausal womenOral
AZD0530
saracatinib
Src tyrosine kinase inhibitorOncologyOral
SB223412
talnetant
Tachykinin receptor/neurokinin 3 (NK3) receptor antagonistCough

Chronic obstructive pulmonary disease

Schizophrenia

Irritable bowel syndrome

Overactive bladder
Oral
(Yes)
SAR115740Transient receptor potential cation channel vanilloid 1 (TRPV1) antagonistAcute and chronic painOral
SSR97225β-Tubulin-binding agent with dual mechanismSolid tumorIntravenous, injectable suspension
AZD2171
cediranib
Vascular endothelial growth factor receptor (VEGFR) 1, 2, and 3 tyrosine kinase inhibitorOncologyOral

*Agents in this table are alphabetized by mechanism of action.

+CNS penetrant: Yes, no or unknown.