SOR-C13

Investigational

Details

Stereochemistry	ABSOLUTE
Molecular Formula	C72H116N20O19
Molecular Weight	1565.814
Optical Activity	UNSPECIFIED
Defined Stereocenters	13 / 13
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

CC(C)C[C@H](NC(=O)[C@H](CC1=CC=CC=C1)NC(=O)[C@H](CCC(O)=O)NC(=O)[C@@H](N)CCCCN)C(=O)N[C@@H](CC2=CN=CN2)C(=O)N3CCC[C@H]3C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CC(O)=O)C(=O)N[C@@H](CC(C)C)C(=O)N4CCC[C@H]4C(=O)N[C@@H](CCCNC(N)=N)C(O)=O

InChI

InChIKey=LGANPTNILMNMES-TVNHODDRSA-N

InChI=1S/C72H116N20O19/c1-39(2)31-48(84-63(102)49(33-42-17-8-7-9-18-42)85-60(99)46(24-25-56(94)95)81-59(98)44(75)19-10-12-26-73)62(101)88-52(34-43-36-78-38-80-43)70(109)92-30-16-23-55(92)67(106)89-53(37-93)65(104)82-45(20-11-13-27-74)61(100)90-58(41(5)6)68(107)86-50(35-57(96)97)64(103)87-51(32-40(3)4)69(108)91-29-15-22-54(91)66(105)83-47(71(110)111)21-14-28-79-72(76)77/h7-9,17-18,36,38-41,44-55,58,93H,10-16,19-35,37,73-75H2,1-6H3,(H,78,80)(H,81,98)(H,82,104)(H,83,105)(H,84,102)(H,85,99)(H,86,107)(H,87,103)(H,88,101)(H,89,106)(H,90,100)(H,94,95)(H,96,97)(H,110,111)(H4,76,77,79)/t44-,45-,46-,47-,48-,49-,50-,51-,52-,53-,54-,55-,58-/m0/s1

HIDE SMILES / InChI

Description
Sources: https://www.cancer.gov/publications/dictionaries/cancer-drug/def/trpv6-calcium-channel-inhibitor-sor-c13 | https://www.soricimed.com/sor-c13.htm

SOR-C13, is a novel, short, synthetic peptide developed from the C-terminal region of soricidin, a proprietary 54 amino acid peptide, discovered by Soricimed Biopharma found in the saliva of the Northern Short-tailed Shrew. SOR-C13 binds with high affinity and selectivity - and disrupts the function of - TRPV6, a calcium channel over-expressed in solid tumor cancers. TRPV6 plays a central role in a biochemical cascade that results in the upregulation of an array of pro-cancerous genes. TRPV6 is considered to be an important target for novel anticancer therapy. SOR-C13 is the first highly specific TRPV6 inhibitor to be identified and to be taken into clinical development. SOR-C13 was effective in inhibition of tumors in animal xenograft models of human ovarian and breast cancer. The ongoing phase I trial studies the side effects and best dose of SOR-C13 in treating patients with solid tumors. The FDA has awarded orphan drug status to SOR-C13 for the treatment of ovarian cancer and for the treatment of pancreatic cancer.

Originator

Approval Year

PubMed

Title	Date	PubMed

Sample Use Guides

In Vivo Use Guide

SOR-C13 was administered IV QD on days 1-3 and 8-10 of a 21-day cycle. Doses were 2.75 and 5.5 mg/kg (20-min infusion) and 1.375, 2.75, 4.13 and 6.2 mg/kg (90-min infusion). The best response was a 27% reduction in a pancreatic tumor with a 55% reduction in CA19-9 levels at 6.2 mg/kg. SOR-C13 was safe and tolerated up to 6.2 mg/kg.

Route of Administration: Intravenous

In Vitro Use Guide

In the presence of 83.5 nM, 417.5 nM, 835 nM and 25 uM SOR-C13 the amplitude of the TRPV6 currents was reduced by 18%, 22%, 24%, and 25%, respectively. The IC50 (Kd) of SOR-C13 was 14 nM.

Name

Type

Language

SOR-C13

Common Name

English

(4S)-5-(((1S)-2-(((1S)-1-(((1S)-2-((2S)-2-(((1S)-2-(((1S)-5-AMINO-1-(((1S)-1-(((1S)-1-(((1S)-1-((2S)-2-(((1S)-1-CARBOXY-4-GUANIDINO-BUTYL)CARBAMOYL)PYRROLIDINE-1-CARBONYL)-3-METHYL-BUTYL)CARBAMOYL)-3-HYDROXY-3-OXO-PROPYL)CARBAMOYL)-2-METHYL-PROPYL)CARBAM

Systematic Name

English

L-ARGININE, L-LYSYL-L-.ALPHA.-GLUTAMYL-L-PHENYLALANYL-L-LEUCYL-L-HISTIDYL-L-PROLYL-L-SERYL-L-LYSYL-L-VALYL-L-.ALPHA.-ASPARTYL-L-LEUCYL-L-PROLYL-

Systematic Name

English

Classification Tree Code System Code

FDA ORPHAN DRUG

526016