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Identification
NameNM-702
Accession NumberDB05505
TypeSmall Molecule
GroupsInvestigational
Description

Nissan Chemical and Taisho have been jointly developing NM-702, a drug for the treatment of arteriosclerosis obliterans.

M-702 is an orally active inhibitor of phosphodiesterase and thromboxane synthetase. In Japan, Phase 2 studies are being conducted for intermittent claudication caused by arteriosclerosis obliterans, intermittent claudication caused by spinal canal stenosis, and asthma. In the USA, a Phase 2 study for intermittent claudication caused by arteriosclerosis obliterans has been successfully completed.
Intermittent claudication is a major symptom of arteriosclerosis obliterans. It is caused by insufficient oxygen supply to exercising muscles in the lower extremities due to decreased blood flow as a result of sclerosis of peripheral arteries. It is estimated that about 6 million people suffer from intermittent claudication in the USA, with only 10 percent of these people currently receiving treatment. Patients with claudication experience significant disability, owing to their exercise limitation. Therapeutic options to improve exercise performance in these patients are limited

Structure
Thumb
SynonymsNot Available
External Identifiers Not Available
Approved Prescription ProductsNot Available
Approved Generic Prescription ProductsNot Available
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International BrandsNot Available
Brand mixturesNot Available
SaltsNot Available
CategoriesNot Available
UNIINot Available
CAS numberNot Available
WeightNot Available
Chemical FormulaNot Available
InChI KeyNot Available
InChINot Available
IUPAC NameNot Available
SMILESNot Available
Taxonomy
ClassificationNot classified
Pharmacology
IndicationInvestigated for use/treatment in peripheral vascular disease.
PharmacodynamicsIntermittent claudication is a major symptom of arteriosclerosis obliterans. It is caused by insufficient oxygen supply to exercising muscles in the lower extremities due to decreased blood flow as a result of sclerosis of peripheral arteries. Patients with claudication experience significant disability, owing to their exercise limitation. Therapeutic options to improve exercise performance in these patients are limited. NM-702 is a novel drug that inhibits phosphodiesterase as well as thromboxane A2 synthase.
Mechanism of actionNM-702 is a novel drug that inhibits phosphodiesterase as well as thromboxane A2 synthase.
Related Articles
AbsorptionNot Available
Volume of distributionNot Available
Protein bindingNot Available
MetabolismNot Available
Route of eliminationNot Available
Half lifeNot Available
ClearanceNot Available
ToxicityNot Available
Affected organismsNot Available
PathwaysNot Available
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
ADMET
Predicted ADMET features
PropertyValueProbability
Human Intestinal AbsorptionNot AvailableNot Available
Blood Brain BarrierNot AvailableNot Available
Caco-2 permeableNot AvailableNot Available
P-glycoprotein substrateNot AvailableNot Available
P-glycoprotein inhibitor INot AvailableNot Available
P-glycoprotein inhibitor IINot AvailableNot Available
Renal organic cation transporterNot AvailableNot Available
CYP450 2C9 substrateNot AvailableNot Available
CYP450 2D6 substrateNot AvailableNot Available
CYP450 3A4 substrateNot AvailableNot Available
CYP450 1A2 substrateNot AvailableNot Available
CYP450 2C9 inhibitorNot AvailableNot Available
CYP450 2D6 inhibitorNot AvailableNot Available
CYP450 2C19 inhibitorNot AvailableNot Available
CYP450 3A4 inhibitorNot AvailableNot Available
CYP450 inhibitory promiscuityNot AvailableNot Available
Ames testNot AvailableNot Available
CarcinogenicityNot AvailableNot Available
BiodegradationNot AvailableNot Available
Rat acute toxicityNot AvailableNot applicable
hERG inhibition (predictor I)Not AvailableNot Available
hERG inhibition (predictor II)Not AvailableNot Available
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
ManufacturersNot Available
PackagersNot Available
Dosage formsNot Available
PricesNot Available
PatentsNot Available
Properties
StateSolid
Experimental PropertiesNot Available
Predicted PropertiesNot Available
Spectra
Mass Spec (NIST)Not Available
Spectra
Spectrum TypeDescriptionSplash Key
References
Synthesis ReferenceNot Available
General References
  1. Ishiwata N, Noguchi K, Kawanishi M, Asakura Y, Hori M, Mitani A, Ito Y, Takahashi K, Nishiyama H, Shudo N, Takahashi S, Takahashi K, Tsuruzoe N, Nakaike S: NT-702 (parogrelil hydrochloride, NM-702), a novel and potent phosphodiesterase inhibitor, improves reduced walking distance and lowered hindlimb plantar surface temperature in a rat experimental intermittent claudication model. Life Sci. 2007 Sep 1;81(12):970-8. Epub 2007 Aug 8. [PubMed:17850826 ]
  2. Brass EP, Jiao J, Hiatt W: Optimal assessment of baseline treadmill walking performance in claudication clinical trials. Vasc Med. 2007 May;12(2):97-103. [PubMed:17615797 ]
  3. Brass EP, Anthony R, Cobb FR, Koda I, Jiao J, Hiatt WR: The novel phosphodiesterase inhibitor NM-702 improves claudication-limited exercise performance in patients with peripheral arterial disease. J Am Coll Cardiol. 2006 Dec 19;48(12):2539-45. Epub 2006 Nov 28. [PubMed:17174195 ]
  4. Kusunoki J, Aragane K, Kitamine T, Yamaura T, Ohnishi H: [Effect of F-1394, a potent and selective inhibitor of acyl-CoA:cholesterol acyltransferase (ACAT), on esterification of cholesterol and basolateral secretion of cholesteryl ester in Caco-2 cells]. Nihon Yakurigaku Zasshi. 1997 Dec;110(6):357-65. [PubMed:9503394 ]
External Links
ATC CodesNot Available
AHFS CodesNot Available
PDB EntriesNot Available
FDA labelNot Available
MSDSNot Available
Interactions
Drug InteractionsNot Available
Food InteractionsNot Available

Targets

Kind
Protein
Organism
Human
Pharmacological action
unknown
General Function:
Thromboxane-a synthase activity
Specific Function:
Not Available
Gene Name:
TBXAS1
Uniprot ID:
P24557
Molecular Weight:
60517.69 Da
References
  1. Berman HM, Westbrook J, Feng Z, Gilliland G, Bhat TN, Weissig H, Shindyalov IN, Bourne PE: The Protein Data Bank. Nucleic Acids Res. 2000 Jan 1;28(1):235-42. [PubMed:10592235 ]
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Drug created on November 18, 2007 11:25 / Updated on September 13, 2013 12:07