ANAMORELIN

Investigational

Details

Stereochemistry	ABSOLUTE
Molecular Formula	C31H42N6O3
Molecular Weight	546.7036
Optical Activity	UNSPECIFIED
Defined Stereocenters	2 / 2
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

CN(C)N(C)C(=O)[C@@]2(CC1=CC=CC=C1)CCCN(C2)C(=O)[C@@H](CC3=CNC4=C3C=CC=C4)NC(=O)C(C)(C)N

InChI

InChIKey=VQPFSIRUEPQQPP-MXBOTTGLSA-N

InChI=1S/C31H42N6O3/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)/t26-,31-/m1/s1

HIDE SMILES / InChI

Molecular Formula	C31H42N6O3
Molecular Weight	546.7036
Charge	0
Count

Stereochemistry	ABSOLUTE
Additional Stereochemistry	No
Defined Stereocenters	2 / 2
E/Z Centers	0
Optical Activity	UNSPECIFIED

Description
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

Targets

Primary Target	Pharmacology	Condition	Potency
Ghrelin receptor 15 Target ID: CHEMBL4616 Sources: http://adisinsight.springer.com/drugs/800021124 https://www.ncbi.nlm.nih.gov/pubmed/24472001	Agonist 2752		0.74 nM [EC50]

Conditions

Condition	Modality	Targets	Highest Phase	Product
Non-small cell lung cancer cachexia 2 Sources: https://clinicaltrials.gov/ct2/show/NCT01395914	Primary		Phase III 665	Unknown Approved Use Unknown

C_max

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

T_1/2

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 Studied dose Dose: 100 mg, 1 times / day Route: oral Route: multiple Dose: 100 mg, 1 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/28472437	unhealthy Health Status: unhealthy Sex: M+F Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/28472437	Other AEs: Hyperglycemia... Other AEs: Hyperglycemia (1.2%) Sources: https://pubmed.ncbi.nlm.nih.gov/28472437

AEs

AE	Significance	Dose	Population
Hyperglycemia	1.2%	100 mg 1 times / day multiple, oral Studied dose Dose: 100 mg, 1 times / day Route: oral Route: multiple Dose: 100 mg, 1 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/28472437	unhealthy Health Status: unhealthy Sex: M+F Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/28472437

Sourcing

Vendor/Aggregator	ID	URL
1PlusChem LLC	1P002QL2	https://www.1pchem.com/search?query=1P002QL2
1PlusChem LLC	1P00GUHJ	https://www.1pchem.com/search?query=1P00GUHJ
AbovChem LLC	HY-14734B	http://www.abovchem.com/pc/en/product_list.aspx?wd=HY-14734B
AChemBlock	10265	http://www.achemblock.com/catalogsearch/result/?q=10265
AK Scientific	3157AH	https://aksci.com/item_detail.php?cat=3157AH
AK Scientific	3444AH	https://aksci.com/item_detail.php?cat=3444AH
AK Scientific	3445AH	https://aksci.com/item_detail.php?cat=3445AH
Alfa Chemistry	ACM249921195	http://www.alfa-chemistry.com/search.aspx?q=ACM249921195
AstaTech	40205	http://astatechinc.com/CPSResult.php?CRNO=40205
BLD Pharm	BD630587	http://www.bldpharm.com/search/Search.html?keyword=BD630587
BLD Pharm	BD630658	http://www.bldpharm.com/search/Search.html?keyword=BD630658
BLD Pharm	BD630916	http://www.bldpharm.com/search/Search.html?keyword=BD630916
BOC Sciences	249921-19-5	http://www.bocsci.com/description.asp?cas=249921-19-5
Chem Scene	CS-1037	http://www.chemscene.com/goproductList/searchProductList?productObj=CS-1037
ChemShuttle	169531	https://www.chemshuttle.com/catalogsearch/result/?q=169531
Debye Scientific	DA-35327	https://www.debyesci.com/index.php?id=product&ext[cno]=DA-35327
eMolecules	266610513	https://orderbb.emolecules.com/search/#?query=266610513
eMolecules	300754452	https://orderbb.emolecules.com/search/#?query=300754452
eMolecules	44811280	https://orderbb.emolecules.com/search/#?query=44811280
eMolecules	44811298	https://orderbb.emolecules.com/search/#?query=44811298
eMolecules	44811505	https://orderbb.emolecules.com/search/#?query=44811505
Excenen	EX-A154	http://www.excenen.com/searchresultlist.php?id=EX-A154
KeyOrganics	AS-75284	http://www.keyorganicsinc.com/bionet/catalogsearch/result?q=AS-75284
mcule	MCULE-1447077543	https://mcule.com/MCULE-1447077543/
mcule	MCULE-5103186823	https://mcule.com/MCULE-5103186823/
mcule	MCULE-7006267405	https://mcule.com/MCULE-7006267405/
MedChem Express	HY-14734	https://www.medchemexpress.com/search.html?q=HY-14734A&ft=&fa=&fp=
MedChem Express	HY-14734A	https://www.medchemexpress.com/search.html?q=HY-14734A&ft=&fa=&fp=
Molnova	M13734	https://www.molnova.com/en/serch-list.html?keywords=M13734
Molnova	M14150	https://www.molnova.com/en/serch-list.html?keywords=M14150
Molnova	M16239	https://www.molnova.com/en/serch-list.html?keywords=M16239
MolPort	MolPort-039-139-550	https://www.molport.com/shop/molecule-link/MolPort-039-139-550
MolPort	MolPort-039-139-551	https://www.molport.com/shop/molecule-link/MolPort-039-139-551
MuseChem	I002848	https://www.musechem.com/product/I002848.html
MuseChem	I003228	https://www.musechem.com/product/I003228.html
PI Chemicals	PI-39497	http://www.pipharm.com/catalog_products/PI-39497.html
Selleck Chemicals	S4980	http://www.selleckchem.com/search.html?searchDTO.searchParam=S4980
ShangHai Biochempartner	BCP000666	http://www.biochempartner.com/search_BCP000666
ShangHai Biochempartner	BCP06108	http://www.biochempartner.com/search_BCP06108
ShangHai Biochempartner	BCP15207	http://www.biochempartner.com/search_BCP15207
ShangHai Biochempartner	BCP23985	http://www.biochempartner.com/search_BCP23985
Toronto Research Chemicals	A637225	https://www.trc-canada.com/product-detail/?CatNum=A637225
Toronto Research Chemicals	A656510	https://www.trc-canada.com/product-detail/?CatNum=A656510
Toronto Research Chemicals	E922033	https://www.trc-canada.com/product-detail/?CatNum=E922033
Toronto Research Chemicals	P139920	https://www.trc-canada.com/product-detail/?CatNum=P139920

PubMed

Title	Date	PubMed
Anamorelin HCl (ONO-7643), a novel ghrelin receptor agonist, for the treatment of cancer anorexia-cachexia syndrome: preclinical profile.	2014-12	25267366
Anamorelin hydrochloride in the treatment of cancer anorexia-cachexia syndrome.	2014-04	24472001

Patents

Sample Use Guides

In Vivo Use Guide

100 mg orally administered daily at least one hour before meal

Route of Administration: Oral

In Vitro Use Guide

Anamorelin showed significant agonist activity on the ghrelin receptor with EC50 value of 0.74 nM

Substance Class	Chemical Created by `admin` on `Mon Mar 31 17:58:25 GMT 2025` Edited by `admin` on `Mon Mar 31 17:58:25 GMT 2025`
Record UNII	DD5RBA1NKF
Record Status	`Validated (UNII)`
Record Version

Download

Name

Type

Language

ONO-7643

Preferred Name

English

ANAMORELIN

Official Name

English

3-PIPERIDINECARBOXYLIC ACID, 1-(2-METHYLALANYL-D-TRYPTOPHYL)-3-(PHENYLMETHYL)-, TRIMETHYLHYDRAZIDE, (3R)-

Common Name

English

ANAMORELIN [MI]

Common Name

English

ST-1291

Code

English

Anamorelin [WHO-DD]

Common Name

English

RC-1291

Code

English

(3R)-1-((2R)-2-((2-AMINO-2-METHYLPROPANOYL)AMINO)-3-(INDOL-3-YL)PROPANOYL)-3-BENZYL-N,N',N'-TRIMETHYLPIPERIDINE-3-CARBOHYDRAZIDE

Systematic Name

English

anamorelin [INN]

Common Name

English

Classification Tree Code System Code

NCI_THESAURUS

C1935