Indication Finder Compounds

NEW -- Indication Finder™:  A Repurposing Hunt

In keeping with our commitment to crowdsourcing and transparency, we invite you to participate in a unique exercise.  The U.S. National Center for Advancing Translational Sciences (NCATS), a division of NIH, has posted a list of 58 clinical stage compounds that were, until recently, being developed by pharmaceutical companies for various indications.  We expect that some of these compounds would be good candidates for Transparency Life Sciences’ approach to drug development.  We need your help in deciding which to pursue and the indications you think could be most promising.  Our Indication Finder™ (TLS-IF) has been developed to assist in this process.  Here's how it works:

• NCATS has linked useful background information to the descriptions of all compounds. Once you have familiarized yourself with the compound and its background, the TLS-IF should take only 10-15 minutes to complete.  There is no limit to how many you can try. 

• The compounds you help select using TLS-IF may become TLS development projects.  If so, they will be developed using Protocol Builder™, TLS’s proprietary crowdsourcing platform for designing better clinical trials.

To get started:
Please review the list and identify the compounds you believe have potential for further development.  Once you have reviewed enough information to assess the compound, complete an Indication Finder for each compound of interest, telling us how you think we should develop the compound along with the basis for your recommendations.  Feel free to provide your views on multiple compounds.  Happy hunting!

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.