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Description
Curator's Comment: Description was created based on several sources, including http://www.tarixorphan.com/ | http://www.fiercepharma.com/partnering/unigene-and-tarix-pharmaceuticals-enter-definitive-licensing-agreement-for-peptelligence

Angiotensin (1-7) [Ang 1-7] is a 7 amino acid peptide generated predominantly from Ang II by the action of Ang-converting enzyme 2. Ang 1-7 can act as a negative modulator of aldosterone secretion in vitro and in vivo. The endogenous heptapeptide angiotensin-(1-7) (Ang-(1-7)) is a RAS component that has a central role in the alternative axis. It is generated by the cleavage of Ang-II by the action of the angiotensin converting enzyme 2 (ACE 2) and acts via interaction with the G-protein coupled receptor Mas. Angiotensin (1-7) induces vasorelaxation through release of NO and prostaglandins, perhaps through activation of a non-AT1, non-AT2 receptor, Mas. Counteracts the vasoconstrictive and proliferative effects of angiotensin II and stimulates vasopressin (anti-diuretic hormone) release in vivo. Clinical uses range from treatment of cardiovascular-related diseases, ocular pathologies, metabolic dysfunctions, brain conditions and degenerative diseases to applications in cell differentiation and hematopoiesis, tumor therapy, acute lung injury, fibrosis, infection, among others. Tarix Orphan is developing TXA127 for rare neuromuscular and connective tissue diseases. TXA127 is a pharmaceutical formulation of the naturally occurring peptide, Angiotensin (1-7). TXA127 has been effective in animal models of Duchenne muscular dystrophy (DMD), Limb-girdle muscular dystrophy (LGMD), congenital muscular dystrophy MDC1A, Marfan syndrome, and Dystrophic Epidermolysis Bullosa (DEB). FDA granted rare pediatric disease designation to TXA127 from Tarix to treat recessive dystrophic epidermolysis bullosa (RDEB). TXA127 has been granted orphan drug status by FDA as a treatment for pulmonary arterial hypertension, to enhance engraftment in patients receiving a stem cell transplant, and for Myelodysplastic Syndrome (MDS). Tarix Orphan has broad IP protection for TXA127 and Orphan Drug Designations (ODDs) have been granted for DMD LGMD and DEB in the U.S., and for DMD in Europe. Tarix Orphan aims to initiate a clinical trials for both DMD and DEB in early 2018 and has an active IND for a Phase II trial in DMD, as well as Fast Track designation for DMD.

CNS Activity

Curator's Comment: Centrally Ang-(1–7) may act as an important neuromodulator, especially in those medullary areas related with the tonic and reflex control of arterial pressure.

Approval Year

PubMed

PubMed

TitleDatePubMed
Angiotensin-(1-7) is an endogenous ligand for the G protein-coupled receptor Mas.
2003 Jul 8
Distinct subsets of unmyelinated primary sensory fibers mediate behavioral responses to noxious thermal and mechanical stimuli.
2009 Jun 2
Angiotensin (1-7) induces MAS receptor internalization.
2011 Aug
Discovery and characterization of alamandine: a novel component of the renin-angiotensin system.
2013 Apr 12
International Union of Basic and Clinical Pharmacology. LXXXVIII. G protein-coupled receptor list: recommendations for new pairings with cognate ligands.
2013 Jul
Pharmacology and signaling of MAS-related G protein-coupled receptors.
2014 Jul
Patents

Sample Use Guides

Treatment of hematologic malignancies: 300mcg/kg/day, subcutaneous injection for up to 28 days
Route of Administration: Other
To investigate whether Ang-(1-7) induces Mas receptor internalization, MasR-YFP transfected HEK 293T cells were incubated with 1 umol/L Ang-(1-7) during different times and the relative cellular distribution of MasR-YFP was observed by laser scanning confocal microscopy. In resting cells, MasR-YFP was mostly localized on the cell membrane and in the endoplasmic reticulum. Treatment of cells with Ang-(1-7) induced redistribution in fluorescence after 5 min stimulation changing the localization of MasR-YFP to intracellular vesicles of various sizes, suggesting internalization of the receptor upon agonist stimulation.
Name Type Language
ANGIOTENSIN 1-7
Common Name English
ANGIOTENSIN FRAGMENT 1-7
Common Name English
5-ILE-ANGIOTENSIN-(1-7)
Common Name English
TXA127
Code English
1-7-ANGIOTENSIN II, 5-L-ISOLEUCINE-
Common Name English
HUMAN ANGIOTENSIN II (1-7)
Common Name English
SH-HEPTAPEPTIDE-13 [INCI]
Common Name English
Angiotensin 1-7 [WHO-DD]
Common Name English
SH-HEPTAPEPTIDE-13
INCI  
INCI  
Official Name English
BF-ANGIOTENSIN 1-7
Brand Name English
TXA-127
Code English
ASP-ARG-VAL-TYR-ILE-HIS-PRO
Common Name English
ANGIOTENSIN PEPTIDE (1-7)
Common Name English
ANGIOTENSIN-(1-7)
Common Name English
ANGIOTENSIN (1-7)
Common Name English
Classification Tree Code System Code
FDA ORPHAN DRUG 144601
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FDA ORPHAN DRUG 400813
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FDA ORPHAN DRUG 308810
Created by admin on Sat Dec 16 01:01:16 GMT 2023 , Edited by admin on Sat Dec 16 01:01:16 GMT 2023
FDA ORPHAN DRUG 508815
Created by admin on Sat Dec 16 01:01:16 GMT 2023 , Edited by admin on Sat Dec 16 01:01:16 GMT 2023
FDA ORPHAN DRUG 546416
Created by admin on Sat Dec 16 01:01:16 GMT 2023 , Edited by admin on Sat Dec 16 01:01:16 GMT 2023
FDA ORPHAN DRUG 295809
Created by admin on Sat Dec 16 01:01:16 GMT 2023 , Edited by admin on Sat Dec 16 01:01:16 GMT 2023
FDA ORPHAN DRUG 129999
Created by admin on Sat Dec 16 01:01:16 GMT 2023 , Edited by admin on Sat Dec 16 01:01:16 GMT 2023
EU-Orphan Drug EU/3/12/1047
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FDA ORPHAN DRUG 412313
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FDA ORPHAN DRUG 411813
Created by admin on Sat Dec 16 01:01:16 GMT 2023 , Edited by admin on Sat Dec 16 01:01:16 GMT 2023
FDA ORPHAN DRUG 345411
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FDA ORPHAN DRUG 402713
Created by admin on Sat Dec 16 01:01:16 GMT 2023 , Edited by admin on Sat Dec 16 01:01:16 GMT 2023
Code System Code Type Description
FDA UNII
IJ3FUK8MOF
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DRUG BANK
DB11720
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ChEMBL
CHEMBL3545347
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PUBCHEM
123805
Created by admin on Sat Dec 16 01:01:16 GMT 2023 , Edited by admin on Sat Dec 16 01:01:16 GMT 2023
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CHEBI
58922
Created by admin on Sat Dec 16 01:01:16 GMT 2023 , Edited by admin on Sat Dec 16 01:01:16 GMT 2023
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NCI_THESAURUS
C68962
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CAS
51833-78-4
Created by admin on Sat Dec 16 01:01:16 GMT 2023 , Edited by admin on Sat Dec 16 01:01:16 GMT 2023
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CHEBI
55438
Created by admin on Sat Dec 16 01:01:16 GMT 2023 , Edited by admin on Sat Dec 16 01:01:16 GMT 2023
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