- Reaction score
- 3,659
Amira AM211 - DP2 antagonist
http://www.medkoo.com/products/8974
MedKoo Cat#: 524179
Name: AM-211
CAS#: 1175526-27-8(AM-211); 1263077-74-2 (AM-211 sodium);
Chemical Formula: C27H27F3N2O4
Exact Mass: 500.19229
Molecular Weight: 500.51
Elemental Analysis: C, 64.79; H, 5.44; F, 11.39; N, 5.60; O, 12.79
Amira Pharmaceuticals Announces Initial Positive Phase 1 Clinical Data for AM211, a Novel Product Candidate for the Treatment of Respiratory Diseases
Pharmacology of AM211, a potent and selective prostaglandin D2 receptor type 2 antagonist that is active in animal models of allergic inflammation.
The prostaglandin D(2) receptor type 2 (DP2) and its ligand, PGD(2), have been implicated in the development of asthma and other inflammatory diseases. The authors evaluated the pharmacodynamics, pharmacokinetics and safety of [2'-(3-benzyl-1-ethyl-ureidomethyl)-6-methoxy-4'-trifluoromethyl-biphenyl-3-yl]-acetic acid sodium salt (AM211), a novel and potent DP2 antagonist, in healthy participants. Single and multiple doses of AM211 demonstrated dose-dependent inhibition of eosinophil shape change in blood with near-complete inhibition observed at trough after dosing 200 mg once daily for 7 days. Maximum plasma concentrations and exposures of AM211 increased in a greater-than-dose-proportional manner after single and multiple dosing. After multiple dosing, the exposures on day 7 were higher than on day 1 with accumulation ratio values ranging from 1.4 to 1.5. Mean terminal half-life values ranged from 14 to 25 hours across the dose range of 100 to 600 mg. AM211 was well tolerated at all doses in both the single- and multiple-dose cohorts. These data support additional clinical studies to evaluate AM211 in asthma and other inflammatory diseases.This sounds great but it doesn't seem to be developed anymore. It was even tested in humans and found to be relatively safe.
I found two slightly differing formulas (or maybe they are the same after all, they seem rotated - I am no chemist). Maybe we could get someone to manufacture this? It sounds pretty good on paper. Surprised Kane isn't offering it.
http://www.medkoo.com/products/8974
MedKoo Cat#: 524179
Name: AM-211
CAS#: 1175526-27-8(AM-211); 1263077-74-2 (AM-211 sodium);
Chemical Formula: C27H27F3N2O4
Exact Mass: 500.19229
Molecular Weight: 500.51
Elemental Analysis: C, 64.79; H, 5.44; F, 11.39; N, 5.60; O, 12.79
Amira Pharmaceuticals Announces Initial Positive Phase 1 Clinical Data for AM211, a Novel Product Candidate for the Treatment of Respiratory Diseases
Pharmacology of AM211, a potent and selective prostaglandin D2 receptor type 2 antagonist that is active in animal models of allergic inflammation.
The prostaglandin D(2) receptor type 2 (DP2) and its ligand, PGD(2), have been implicated in the development of asthma and other inflammatory diseases. The authors evaluated the pharmacodynamics, pharmacokinetics and safety of [2'-(3-benzyl-1-ethyl-ureidomethyl)-6-methoxy-4'-trifluoromethyl-biphenyl-3-yl]-acetic acid sodium salt (AM211), a novel and potent DP2 antagonist, in healthy participants. Single and multiple doses of AM211 demonstrated dose-dependent inhibition of eosinophil shape change in blood with near-complete inhibition observed at trough after dosing 200 mg once daily for 7 days. Maximum plasma concentrations and exposures of AM211 increased in a greater-than-dose-proportional manner after single and multiple dosing. After multiple dosing, the exposures on day 7 were higher than on day 1 with accumulation ratio values ranging from 1.4 to 1.5. Mean terminal half-life values ranged from 14 to 25 hours across the dose range of 100 to 600 mg. AM211 was well tolerated at all doses in both the single- and multiple-dose cohorts. These data support additional clinical studies to evaluate AM211 in asthma and other inflammatory diseases.This sounds great but it doesn't seem to be developed anymore. It was even tested in humans and found to be relatively safe.
I found two slightly differing formulas (or maybe they are the same after all, they seem rotated - I am no chemist). Maybe we could get someone to manufacture this? It sounds pretty good on paper. Surprised Kane isn't offering it.