"目录号: HY-14734B
Anamorelin(RC1291; ONO-7643)延胡索酸盐是口服活性的饥饿素受体激动剂。
相关产品
Anamorelin-Ibutamoren Mesylate-Alexamorelin-AZP-531-GHRP-2 metabolite 1-Capromorelin Tartrate-Examorelin-TC-G-1008-
生物活性
Description
Anamorelin Fumarate is a novelghrelin receptoragonist withEC50value of 0.74 nM in the FLIPR assay.
IC50& Target
Ki: 0.7 nM (ghrelin receptor)[1]
EC50: 0.74 nM (ghrelin receptor)[1]
In Vitro
In the FLIPR assay, Anamorelin (ANAM) shows significant agonist activity on the ghrelin receptor, with EC50value of 0.74 nM. No significant antagonist activity is observed with Anamorelin at concentrations of up to 1,000 nM. In the binding experiments, Anamorelin binds to the ghrelin receptor with a binding affinity constant (Ki) of 0.70 nM. In the competition assay with radiolabeled ibutamoren (35S-MK-677; another ghrelin receptor agonist) Anamorelin (ANAM) is also found to bind with high affinity to the ghrelin receptor (IC50=0.69 nM). In rat pituitary cells incubated with Anamorelin, there is a dose-dependent stimulatory effect on GH release and the potency (EC50) is 1.5 nM. Anamorelin is screened for activity against a set of over 100 receptors, ion channels, transporters, and enzymes. Anamorelin demonstrates binding to the tachykinin neurokinin 2 (NK2) site (IC50=0.021 μM); however, a subsequent NK2functional assay demonstrates no functional activity[1].?
In Vivo
In rats, Anamorelin (ANAM) at an oral dose of 3, 10, or 30 mg/kg once daily significantly increases both food intake and body weight from Day 2 to Day 7 of treatment compared with the vehicle control. The cumulative change in food intake and weight gain increases dose-dependently, and these changes are significant at all dose levels (P<0.05) compared to the control. Administration of Anamorelin at a single oral dose of 3, 10, or 30 mg/kg induces a dose-dependent increase in plasma GH levels and GH AUC0-6hin rats[1].
Clinical Trial
M.D. Anderson Cancer Center-Helsinn Healthcare SA
Malignant Neoplasms of Independent (Primary) Multiple Sites-Advanced Cancer-Metastatic or Recurrent Incurable Solid Tumors
February 8, 2017
Phase 2
Helsinn Therapeutics (U.S.), Inc
Cachexia-Non-Small Cell Lung Cancer
July 2011
Phase 3
Helsinn Therapeutics (U.S.), Inc
Cachexia-Non-Small Cell Lung Cancer
July 2011
Phase 3
Helsinn Therapeutics (U.S.), Inc
Cachexia-Non-Small Cell Lung Cancer
July 2011
Phase 3
Helsinn Therapeutics (U.S.), Inc
Carcinoma, Non-Small-Cell Lung
March 2008
Phase 2
VA Office of Research and Development-Helsinn Therapeutics (U.S.), Inc
Cancer Cachexia
June 2012
Phase 2
M.D. Anderson Cancer Center-Helsinn Healthcare SA
Malignant Neoplasms of Independent (Primary) Multiple Sites-Advanced Cancer-Metastatic or Recurrent Incurable Solid Tumors
February 8, 2017
Phase 2
Helsinn Therapeutics (U.S.), Inc
Cachexia-Non-Small Cell Lung Cancer
July 2011
Phase 3
Helsinn Therapeutics (U.S.), Inc
Cachexia-Non-Small Cell Lung Cancer
July 2011
Phase 3
Helsinn Therapeutics (U.S.), Inc
Cachexia-Non-Small Cell Lung Cancer
July 2011
Phase 3
Helsinn Therapeutics (U.S.), Inc
Carcinoma, Non-Small-Cell Lung
March 2008
Phase 2
VA Office of Research and Development-Helsinn Therapeutics (U.S.), Inc
Cancer Cachexia
June 2012
Phase 2
Helsinn Therapeutics (U.S.), Inc
Cancer Cachexia
September 2006
Phase 2
Helsinn Therapeutics (U.S.), Inc
Cancer Cachexia
November 2005
Phase 2
Helsinn Therapeutics (U.S.), Inc
Cancer Cachexia
June 2005
Phase 2
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References
