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Library of Industry-Provided Agents

The private sector holds many of the agents and data needed for efficient drug rescue and repurposing. However, innovative ideas for new uses of these resources come from a variety of organizations, including NIH and the broader biomedical research community. As such, partnerships and collaborations are critical to this research. Through the Discovering New Therapeutic Uses for Existing Molecules pilot program, companies will provide researchers with access to the compounds and related data.

These compounds and biologics have undergone significant pre-clinical and Phase I testing and are ready for additional testing in humans. Making information about these promising agents available to the research community gives scientists an opportunity to explore potential new therapeutic uses in previously unexplored disease areas. Learn more about how to apply to the Therapeutics Discovery program.

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.