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 Information | Mechanism 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 | Hypercholesterolemia | Oral |
SSR149744C 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 senicapoc (ICA-17043) | Calcium-activated potassium channel blocker (KCa3.1), intermediate-conductance | Sickle cell disease Asthma | Oral |
ABT-639 | Calcium channel, voltage-gated (Cav3.2, T-type) blocker | Pain | Oral (Yes) |
CP-945598 otenabant | Cannabinoid receptor 1 (CB1) antagonist | Obesity | Oral (Yes) |
LY2828360 | Cannabinoid receptor 2 (CB2) agonist | Osteoarthritis pain | Oral (Yes) |
AZD1981 | Chemoattractant receptor-homologous molecule expressed on Th2 cells (CRTh2)/prostaglandin D2 (DP2) receptor antagonist | Asthma Chronic obstructive pulmonary disease | Oral |
SSR150106 | Chemokine receptor antagonist (TNFα release) | Rheumatoid arthritis pain | Oral |
AZD2423 | Chemokine (C-C motif) receptor 2 (CCR2) antagonist | Chronic obstructive pulmonary disease Pain | Oral |
PF-04136309 | Chemokine (C-C motif) receptor 2 (CCR2) antagonist | Chronic osteoarthritis pain | Oral (No) |
CE-326597 | Cholecystokinin 1 receptor (CCK-1R) (or CCKA receptor) agonist | Obesity in type II diabetes | Oral |
BMS-562086 pexacerfont | Corticotropin-releasing factor 1 (CRF1) receptor antagonist | Major depressive disorder Generalized anxiety disorder Irritable bowel syndrome | Oral (Yes) |
JNJ-39269646 | Fast dissociating D2/D3/5-HT6 antagonist | Schizophrenia | Oral (Yes) |
ZD4054 zibotentan | Endothelin receptor A (ETA) antagonist | Oncology Pulmonary artery hypertension | Oral |
PF-00913086 prinaberel (ERB-041) | Estrogen receptor β (ERβ, ESR2) agonist/nuclear receptor 3A2 (NR3A2) agonist | Endometriosis | Oral |
LY500307 | Estrogen receptor β (ERβ, ESR2) agonist/nuclear receptor 3A2 (NR3A2) agonist | Benign prostatic hyperplasia Lower urinary tract symptoms | Oral |
XRP0038 Riferminogene pecaplasmid, NV1FGF, temusi | Non-viral fibroblast growth factor 1 (NV1FGF) | Critical limb ischemia | Intramuscular (No) |
AZD7325 | γ-Aminobutyric acid (GABA) A receptor, alpha 2 (GABAA α2) agonist | Generalized anxiety disorder | Oral (Yes) |
AZD3355 lesogaberan | γ-Aminobutyric acid (GABA) B receptor, 1 (GABAB1) agonist | Gastroesophageal reflux disease | Oral |
PF-05190457 | Ghrelin receptor (growth hormone secretagogue 1a receptor, GHS-1aR) inverse agonist, competitive antagonist | Type II diabetes | Oral (Yes) |
AZD1656 | Glucokinase (GK) activator | Diabetes | Oral |
BMS-820132 | Glucokinase (GK) activator | Type II diabetes | Oral |
PF-03463275 | Glycine transporter 1 (GlyT1) inhibitor Solute carrier family 6 (neurotransmitter transporter, glycine), member 9 (SLC6A9) inhibitor | Schizophrenia | Oral (Yes) |
HMR1766 ataciguat | Soluble guanylate cyclase (sGC) activator | Angina pectoris Peripheral artery disease Neuropathic pain | Oral |
GSK1004723 | Histamine H1/H3 receptor antagonist | Allergic rhinitis | Topical (No) |
GSK835726 | Histamine H1/H3 receptor antagonist | Allergic rhinitis | Oral (No) |
ABT-288 | Histamine H3 receptor antagonist | Cognition (cognitive deficits of schizophrenia) | Oral (Yes) |
PF-03654746 | Histamine H3 receptor antagonist | Narcolepsy Cognition Attention deficit hyperactivity disorder Allergic rhinitis | Oral (Yes) |
CE-210666 | 5-Hydroxytryptamine 1B receptor (5-HT1B) antagonist | Depression | Oral (Yes) |
CP-448187 elzasonan | 5-Hydroxytryptamine 1B receptor (5-HT1B) antagonist | Depression | Oral (Yes) |
PH-670187 dermaciclane, EGIS-3886 | 5-Hydroxytryptamine 2A/2C receptor (5-HT2A/2C) antagonist | Generalized anxiety disorder | Oral (Yes) |
PF-04995274 | 5-Hydroxytryptamine 4 receptor (5-HT4) partial agonist | Gastroesophageal reflux disease Alzheimer's disease | Oral (Yes) |
JNJ-18038683 | 5-Hydroxytryptamine 7 receptor (5-HT7) antagonist | Major depressive disorder | Oral (Yes) |
LY2590443 | 5-Hydroxytryptamine 7A receptor (5-HT7A) antagonist | Migraine | Oral |
MEDI2338 | Interleukin-18 (IL-18) inhibitor | Chronic obstructive pulmonary disease Coronary heart disease | Intravenous, subcutaneous |
PF-04191834 | 5-Lipoxygenase (5-LO) inhibitor | Asthma Chronic osteoarthritis pain | Oral (Yes) |
SD-7300 (SC-81490) | Matrix metalloproteinase 2, 9, and 13 (MMP-2, -9, -13) inhibitor | Post-myocardial infarction cardiac remodeling Disease-modifying osteoarthritis drug | Oral |
AZD1236 | Matrix metalloproteinase 9|12 (MMP9|MMP12) inhibitor | Chronic obstructive pulmonary disease | Oral |
BMS-830216 | Melanin-concentrating hormone 1 (MCH1) receptor antagonist | Obesity | Oral (Yes) |
AZD5904 | Myeloperoxidase (MPO) inhibitor | Chronic obstructive pulmonary disease Multiple sclerosis | Oral |
SAR103168 | Multi-kinase inhibitor | Liquid tumors (acute myeloid leukemia) | Intravenous |
ABT-089 | Nicotinic acetylcholine receptor (nAChR) partial agonist (α4β2* subtypes) | Alzheimer's disease Attention deficit hyperactivity disorder | Oral (Yes) |
CP-601927 | Nicotinic acetylcholine receptor α4β2 (α4β2 nAChR) partial agonist | Multiple CNS | Oral (Yes) |
AZD0328 | Nicotinic acetylcholine receptor alpha 7 (α7 nAChR) agonist | Cognitive impairment | Oral (Yes) |
JNJ-39393406 | Nicotinic acetylcholine receptor, α7 (α7nAChR) positive allosteric modulator | Cognitive impairment in schizophrenia | Oral (Yes) |
GW274150 | Inducible nitric oxide synthase (iNOS) inhibitor | Migraine (acute and prophylaxis) Asthma Rheumatoid arthritis Sepsis | Oral (Poor) |
SD-6010 (SC-84250) | Inducible nitric oxide synthase (iNOS) inhibitor | Asthma Osteoarthritis pain Disease-modifying osteoarthritis drug | Oral |
AZD7268 | δ Opioid receptor agonist | Anxiety Depression | Oral (Yes) |
AVE8134 | Peroxisome proliferator-activated receptor α (PPARα)/nuclear receptor 1C1 (NR1C1) agonist | Type II diabetes | Oral |
AVE0847 | Peroxisome proliferator-activated receptor α/γ (PPARα/γ)/nuclear receptor 1C1/1C3 (NR1C1/1C3) agonist | Type II diabetes | Oral |
PF-05019702 (PRA-27) | Progesterone receptor (PR) antagonist/nuclear receptor 3C3C (NRC3C) antagonist | Endometriosis | Oral |
AZD9056 | Purinergic receptor 2X, ligand-gated ion channel, 7 (P2X7) antagonist | Chronic obstructive pulmonary disease Crohn’s disease Osteoarthritis Rheumatoid arthritis | Oral |
LY2245461 | Selective estrogen receptor modulator (SERM) | Hot flashes in postmenopausal women | Oral |
AZD0530 saracatinib | Src tyrosine kinase inhibitor | Oncology | Oral |
SB223412 talnetant | Tachykinin receptor/neurokinin 3 (NK3) receptor antagonist | Cough Chronic obstructive pulmonary disease Schizophrenia Irritable bowel syndrome Overactive bladder | Oral (Yes) |
SAR115740 | Transient receptor potential cation channel vanilloid 1 (TRPV1) antagonist | Acute and chronic pain | Oral |
SSR97225 | β-Tubulin-binding agent with dual mechanism | Solid tumor | Intravenous, injectable suspension |
AZD2171 cediranib | Vascular endothelial growth factor receptor (VEGFR) 1, 2, and 3 tyrosine kinase inhibitor | Oncology | Oral |
*Agents in this table are alphabetized by mechanism of action.
+CNS penetrant: Yes, no or unknown.
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