TEPRENONE

Description
Sources: http://www.shijiebiaopin.net/upload/product/201431323032020.pdf
Curator's Comment: Description was created based on several sources including http://www.ncbi.nlm.nih.gov/pubmed/26345206

Tetraprenylacetone (Geranylgeranylacetone) is an anti-peptic ulcer drug developed and approved in Japan in 1984. Tetraprenylacetone is shown to suppress H. pylori induced tissue and cell injury and inflammatory reaction, so it is expected to show beneficial effects on H. pylori-infected tissues. Tetraprenylacetone is used to treat patients suffering from peptic ulcers and gastritis. In Japan it is sold under the brand name Selbex.

CNS Activity

Originator

Approval Year

Targets

Primary Target	Pharmacology	Potency
Apoptosis 155 Target ID: map04210 Sources: http://www.ncbi.nlm.nih.gov/pubmed/27470333	Activator 1430
Chaperone protein DnaK Helicobacter pylori NCTC 11637 ATCC 43504 2 Target ID: Chaperone protein DnaK Helicobacter pylori NCTC 11637 ATCC 43504 Sources: http://www.ncbi.nlm.nih.gov/pubmed/26345206	Modulator 828	0.076 mM [Kd]
Heat shock 70 kDa protein 1 6 Target ID: CHEMBL5460 Sources: http://www.ncbi.nlm.nih.gov/pubmed/26345206	Modulator 828	0.02 mM [Kd]
Interleukin-8 3 Target ID: CHEMBL2157 Sources: http://www.ncbi.nlm.nih.gov/pubmed/15068414	Inhibitor 8297
mucin 5AC, oligomeric mucus/gel-forming 2 Target ID: 682837.0 Gene Symbol: Muc5ac Sources: http://www.ncbi.nlm.nih.gov/pubmed/16240224	Activator 1430
mucin 6, oligomeric mucus/gel-forming 2 Target ID: 282586.0 Gene Symbol: Muc6 Sources: http://www.ncbi.nlm.nih.gov/pubmed/16240224	Activator 1430
Hsp70 [Homo sapiens] 2 Target ID: Hsp70 [Homo sapiens] Sources: http://www.ncbi.nlm.nih.gov/pubmed/17684364	Activator 1430

Conditions

Condition	Modality	Targets	Highest Phase	Product
Gastric ulcer 67 Sources: http://www.shijiebiaopin.net/upload/product/201431323032020.pdf	Primary		Approved 8429	Selbex Approved Use Improvement of gastric mucosal lesions (erosion, hemorrhage, redness and edema) in the following diseases: Acute gastritis and acute exacerbation stage of chronic gastritis and Gastric ulcers Launch Date 1984
Gastritis 45 Sources: http://www.shijiebiaopin.net/upload/product/201431323032020.pdf	Primary		Approved 8429	Selbex Approved Use Improvement of gastric mucosal lesions (erosion, hemorrhage, redness and edema) in the following diseases: Acute gastritis and acute exacerbation stage of chronic gastritis and Gastric ulcers Launch Date 1984

PubMed

Title	Date	PubMed
Suppression of Alzheimer's disease-related phenotypes by geranylgeranylacetone in mice.	2013	24098472
Geranylgeranylacetone induces apoptosis via the intrinsic pathway in human melanoma cells.	2016 Aug	27470333

Patents

Sample Use Guides

In Vivo Use Guide

Capsules 50 mg: The usual adult dosage for oral use is 3 capsules (150 mg of teprenone) daily in three divided doses after meals. The dosage may be adjusted depending on the patient’s age and symptoms. Fine Granules 10%: The usual adult dosage for oral use is 1.5 g (150 mg of teprenone) daily in three divided doses after meals. The dosage may be adjusted depending on the patient’s age and symptoms.

Route of Administration: Oral

In Vitro Use Guide

Human melanoma cell lines G361, SK-MEL-2, and SK-MEL-5 were treated with GGA (Tetraprenylacetone) at various doses (1-100uM). GGA significantly reduced the viability of G361, SK-MEL-2, and SK-MEL-5 human melanoma cells at concentrations above 10uM.

Name

Type

Language

TEPRENONE

Official Name

English

teprenone [INN]

Common Name

English

SELBEX

Brand Name

English

Teprenone [WHO-DD]

Common Name

English

TEPRENONE [MART.]

Common Name

English

TEPRENONE [JAN]

Common Name

English

TEPRENONE [INCI]

Common Name

English

GERANYLGERANYLACETONE

Common Name

English

5,9,13,17-NONADECATETRAEN-2-ONE, 6,10,14,18-TETRAMETHYL-, MIXTURE OF (5Z,9E,13E) AND ALL TRANS (5E,9E,13E)

Common Name

English

5,9,13,17-NONADECATETRAEN-2-ONE, 6,10,14,18-TETRAMETHYL-

Common Name

English

TEPRENONE [MI]

Common Name

English

E-0671

Code

English

Classification Tree Code System Code

FDA ORPHAN DRUG

743920