Details
Stereochemistry | ABSOLUTE |
Molecular Formula | 2C29H35N4O5.Ca |
Molecular Weight | 1079.302 |
Optical Activity | UNSPECIFIED |
Defined Stereocenters | 2 / 2 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
[Ca++].CC(C)(C)C(=O)CN1C2=CC=CC=C2N(C[C@@H](NC(=O)NC3=CC(=CC=C3)C([O-])=O)C1=O)C4CCCCC4.CC(C)(C)C(=O)CN5C6=CC=CC=C6N(C[C@@H](NC(=O)NC7=CC(=CC=C7)C([O-])=O)C5=O)C8CCCCC8
InChI
InChIKey=DLRNGUKRKXEPEL-LJWMURKVSA-L
InChI=1S/2C29H36N4O5.Ca/c2*1-29(2,3)25(34)18-33-24-15-8-7-14-23(24)32(21-12-5-4-6-13-21)17-22(26(33)35)31-28(38)30-20-11-9-10-19(16-20)27(36)37;/h2*7-11,14-16,21-22H,4-6,12-13,17-18H2,1-3H3,(H,36,37)(H2,30,31,38);/q;;+2/p-2/t2*22-;/m11./s1
DescriptionSources: https://www.ncbi.nlm.nih.gov/pubmed/20006921Curator's Comment: description was created based on several sources, including:
http://adisinsight.springer.com/drugs/800016682 | http://www.zeria.co.jp/english/comp/co_0501.html |
Sources: https://www.ncbi.nlm.nih.gov/pubmed/20006921
Curator's Comment: description was created based on several sources, including:
http://adisinsight.springer.com/drugs/800016682 | http://www.zeria.co.jp/english/comp/co_0501.html |
Nastorazepide (Z-360) is a selective, orally available, gastrin/cholecystokinin 2 (CCK-2) receptor antagonist with potential antineoplastic activity. Z-360 binds to the gastrin/CCK-2 receptor, thereby preventing receptor activation by gastrin, a peptide hormone frequently associated with the proliferation of gastrointestinal and pancreatic tumor cells. It is currently under development as a therapeutic drug for pancreatic cancer, gastroesophageal reflux disease and peptic ulcers. The most commonly reported adverse events were nausea, abdominal pain, vomiting and fatigue.
Originator
Sources: http://adisinsight.springer.com/drugs/800016682
Curator's Comment: http://www.zeria.co.jp/english/comp/co_0501.html
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
---|---|---|---|
Target ID: CHEMBL298 Sources: http://www.zeria.co.jp/english/comp/co_0501.html |
0.47 nM [Kd] |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
---|---|---|---|---|
Primary | Unknown Approved UseUnknown |
|||
Primary | Unknown Approved UseUnknown |
|||
Sources: DOI: 10.1016/S0016-5085(08)81545-4 http://www.pharmacodia.com/web/drug/1_1566.html |
Primary | Unknown Approved UseUnknown |
Cmax
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
4434 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/20006921/ |
120 mg single, oral dose: 120 mg route of administration: Oral experiment type: SINGLE co-administered: |
NASTORAZEPIDE CALCIUM plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
|
6756 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/20006921/ |
240 mg single, oral dose: 240 mg route of administration: Oral experiment type: SINGLE co-administered: |
NASTORAZEPIDE CALCIUM plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
AUC
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
18600 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/20006921/ |
120 mg single, oral dose: 120 mg route of administration: Oral experiment type: SINGLE co-administered: |
NASTORAZEPIDE CALCIUM plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
|
24030 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/20006921/ |
240 mg single, oral dose: 240 mg route of administration: Oral experiment type: SINGLE co-administered: |
NASTORAZEPIDE CALCIUM plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
T1/2
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
4.17 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/20006921/ |
120 mg single, oral dose: 120 mg route of administration: Oral experiment type: SINGLE co-administered: |
NASTORAZEPIDE CALCIUM plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
|
5.5 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/20006921/ |
240 mg single, oral dose: 240 mg route of administration: Oral experiment type: SINGLE co-administered: |
NASTORAZEPIDE CALCIUM plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
Overview
CYP3A4 | CYP2C9 | CYP2D6 | hERG |
---|---|---|---|
OverviewOther
Other Inhibitor | Other Substrate | Other Inducer |
---|---|---|
Drug as perpetrator
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
no | ||||
no | ||||
no | ||||
no | ||||
no | ||||
no | ||||
no | ||||
no | ||||
no | ||||
no | ||||
no | ||||
no | ||||
no | ||||
weak [IC50 10 uM] | ||||
yes [IC50 1 uM] |
Drug as victim
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
no | ||||
yes |
Sample Use Guides
In Vivo Use Guide
Sources: https://clinicaltrials.gov/ct2/show/NCT02117258
60, 120 or 240 mg, twice daily (28-day cycle).
Route of Administration:
Oral
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/21839751
In PANC-1 cells, gemcitabineinduced expression of HIF-1alpha gene was suppressed by treatment
with 0.1 μM Z-360.
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Classification Tree | Code System | Code | ||
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NCI_THESAURUS |
C129824
Created by
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DTXSID40187905
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C61329
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343326-69-2
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10170574
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GZ3I1DMI8Q
Created by
admin on Sat Dec 16 10:31:20 GMT 2023 , Edited by admin on Sat Dec 16 10:31:20 GMT 2023
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ACTIVE MOIETY
SUBSTANCE RECORD