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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 of SOR-C13

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

Molecular Formula C72H116N20O19
Molecular Weight 1565.814
Charge 0
Count
Stereochemistry ABSOLUTE
Additional Stereochemistry No
Defined Stereocenters 13 / 13
E/Z Centers 4
Optical Activity UNSPECIFIED

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.

Approval Year

PubMed

PubMed

TitleDatePubMed
Erratum to: First-in-human phase I study of SOR-C13, a TRPV6 calcium channel inhibitor, in patients with advanced solid tumors.
2017 Jun

Sample Use Guides

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 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.
Substance Class Chemical
Created
by admin
on Sat Dec 16 11:29:01 GMT 2023
Edited
by admin
on Sat Dec 16 11:29:01 GMT 2023
Record UNII
C79B5A73C4
Record Status Validated (UNII)
Record Version
  • Download
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
Created by admin on Sat Dec 16 11:29:01 GMT 2023 , Edited by admin on Sat Dec 16 11:29:01 GMT 2023
FDA ORPHAN DRUG 505215
Created by admin on Sat Dec 16 11:29:01 GMT 2023 , Edited by admin on Sat Dec 16 11:29:01 GMT 2023
Code System Code Type Description
NCI_THESAURUS
C101525
Created by admin on Sat Dec 16 11:29:01 GMT 2023 , Edited by admin on Sat Dec 16 11:29:01 GMT 2023
PRIMARY
CAS
1187852-48-7
Created by admin on Sat Dec 16 11:29:01 GMT 2023 , Edited by admin on Sat Dec 16 11:29:01 GMT 2023
PRIMARY
DRUG BANK
DB15366
Created by admin on Sat Dec 16 11:29:01 GMT 2023 , Edited by admin on Sat Dec 16 11:29:01 GMT 2023
PRIMARY
FDA UNII
C79B5A73C4
Created by admin on Sat Dec 16 11:29:01 GMT 2023 , Edited by admin on Sat Dec 16 11:29:01 GMT 2023
PRIMARY
PUBCHEM
121596688
Created by admin on Sat Dec 16 11:29:01 GMT 2023 , Edited by admin on Sat Dec 16 11:29:01 GMT 2023
PRIMARY
Related Record Type Details
TARGET -> INHIBITOR
INHIBITOR
Related Record Type Details
ACTIVE MOIETY
Originator: Soricimed Biopharma; Class: Antineoplastic, Peptide; Mechanism of Action: TRPV6 protein inhibitor; Orphan Drug Status: Yes for Ovarian cancer; On Fast track: No; New Molecular Entity: Yes; Highest Development Phases: Phase I for Ovarian cancer, Solid tumours; Most Recent Events: 19 Jul 2016 Final adverse events and efficacy data from a phase I trial in Solid tumours presented at the 107th Annual Meeting of the American Association for Cancer Research (AACR-2016), 08 Mar 2016 SOR C13 receives Orphan Drug status for Ovarian cancer (Late-stage disease) in USA, 23 Feb 2016 Efficacy and adverse events data from a phase I trial in Solid tumours released by Soricimed
ACTIVE MOIETY
Official Title: Phase I, Open-label, Dose Escalation Study to Assess Safety and Tolerability of SOR-C13 in Subjects With Advanced Solid Tumors Commonly Known to Express the TRPV6 Ion Channel Purpose: The purpose of this study is to determine the safety and tolerability of the drug SOR-C13 when given as an intravenous infusion in patients with ovarian cancer or other cancers known to over express the TRPV6 calcium channel.