Details
Stereochemistry | ABSOLUTE |
Molecular Formula | C31H42N6O3.ClH |
Molecular Weight | 583.165 |
Optical Activity | UNSPECIFIED |
Defined Stereocenters | 2 / 2 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
Cl.CN(C)N(C)C(=O)[C@@]2(CC1=CC=CC=C1)CCCN(C2)C(=O)[C@@H](CC3=CNC4=CC=CC=C34)NC(=O)C(C)(C)N
InChI
InChIKey=VFYAEUWJFGTGGO-GHTUPXNNSA-N
InChI=1S/C31H42N6O3.ClH/c1-30(2,32)28(39)34-26(18-23-20-33-25-15-10-9-14-24(23)25)27(38)37-17-11-16-31(21-37,29(40)36(5)35(3)4)19-22-12-7-6-8-13-22;/h6-10,12-15,20,26,33H,11,16-19,21,32H2,1-5H3,(H,34,39);1H/t26-,31-;/m1./s1
DescriptionSources: http://adisinsight.springer.com/drugs/800021124Curator's Comment: https://www.ncbi.nlm.nih.gov/pubmed/26386985
https://www.ncbi.nlm.nih.gov/pubmed/24472001
https://www.cancer.gov/publications/dictionaries/cancer-drug?cdrid=460131
Sources: http://adisinsight.springer.com/drugs/800021124
Curator's Comment: https://www.ncbi.nlm.nih.gov/pubmed/26386985
https://www.ncbi.nlm.nih.gov/pubmed/24472001
https://www.cancer.gov/publications/dictionaries/cancer-drug?cdrid=460131
Anamorelin is a first-in-class, orally active ghrelin receptor agonist that binds and stimulates the growth hormone secretagogue receptor centrally, thereby mimicking the appetite-enhancing and anabolic effects of ghrelin. Anamorelin is under development by Helsinn Therapeutics for the treatment of cancer cachexia and anorexia. Anamorelin has completed phase III clinical trials for the treatment of cancer cachexia and anorexia associated with non-small-cell lung carcinoma. Results of the studies were positive, and the drug is now in preregistration with the European Medicines Agency.
CNS Activity
Originator
Approval Year
Cmax
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
80.6 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/26640742/ |
25 mg single, oral dose: 25 mg route of administration: Oral experiment type: SINGLE co-administered: |
ANAMORELIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
184 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/26640742/ |
25 mg single, oral dose: 25 mg route of administration: Oral experiment type: SINGLE co-administered: |
ANAMORELIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE food status: FASTED |
AUC
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
197 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/26640742/ |
25 mg single, oral dose: 25 mg route of administration: Oral experiment type: SINGLE co-administered: |
ANAMORELIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
366 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/26640742/ |
25 mg single, oral dose: 25 mg route of administration: Oral experiment type: SINGLE co-administered: |
ANAMORELIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE food status: FASTED |
T1/2
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
7.03 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/26640742/ |
25 mg single, oral dose: 25 mg route of administration: Oral experiment type: SINGLE co-administered: |
ANAMORELIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
6.08 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/26640742/ |
25 mg single, oral dose: 25 mg route of administration: Oral experiment type: SINGLE co-administered: |
ANAMORELIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE food status: FASTED |
Doses
Dose | Population | Adverse events |
---|---|---|
100 mg 1 times / day multiple, oral (unknown) Studied dose Dose: 100 mg, 1 times / day Route: oral Route: multiple Dose: 100 mg, 1 times / day Sources: |
unhealthy n = 343 Health Status: unhealthy Condition: NSCLC Sex: M+F Food Status: UNKNOWN Population Size: 343 Sources: |
Other AEs: Hyperglycemia... |
AEs
AE | Significance | Dose | Population |
---|---|---|---|
Hyperglycemia | 1.2% | 100 mg 1 times / day multiple, oral (unknown) Studied dose Dose: 100 mg, 1 times / day Route: oral Route: multiple Dose: 100 mg, 1 times / day Sources: |
unhealthy n = 343 Health Status: unhealthy Condition: NSCLC Sex: M+F Food Status: UNKNOWN Population Size: 343 Sources: |
Sample Use Guides
In Vivo Use Guide
Sources: https://clinicaltrials.gov/ct2/show/NCT01387269
100 mg orally administered daily at least one hour before meal
Route of Administration:
Oral
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/25267366
Anamorelin showed significant agonist activity on the ghrelin receptor with EC50 value of 0.74 nM
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Classification Tree | Code System | Code | ||
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NCI_THESAURUS |
C1935
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ACTIVE MOIETY
SUBSTANCE RECORD