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Details

Stereochemistry ABSOLUTE
Molecular Formula C40H66N2O9
Molecular Weight 718.96
Optical Activity UNSPECIFIED
Defined Stereocenters 10 / 10
E/Z Centers 2
Charge 0

SHOW SMILES / InChI
Structure of E7107

SMILES

[H][C@@]1(O[C@@H]1C[C@@](C)(O)\C=C\C=C(/C)[C@@]2([H])OC(=O)C[C@H](O)CC[C@@](C)(O)[C@@H](OC(=O)N3CCN(CC3)C4CCCCCC4)\C=C\[C@@H]2C)[C@H](C)[C@@H](O)CC

InChI

InChIKey=MNOMBFWMICHMKG-MGYWSNOQSA-N
InChI=1S/C40H66N2O9/c1-7-32(44)29(4)37-33(49-37)26-39(5,47)19-12-13-27(2)36-28(3)16-17-34(40(6,48)20-18-31(43)25-35(45)51-36)50-38(46)42-23-21-41(22-24-42)30-14-10-8-9-11-15-30/h12-13,16-17,19,28-34,36-37,43-44,47-48H,7-11,14-15,18,20-26H2,1-6H3/b17-16+,19-12+,27-13+/t28-,29+,31+,32-,33+,34-,36+,37+,39-,40+/m0/s1

HIDE SMILES / InChI

Molecular Formula C40H66N2O9
Molecular Weight 718.96
Charge 0
Count
MOL RATIO 1 MOL RATIO (average)
Stereochemistry ABSOLUTE
Additional Stereochemistry No
Defined Stereocenters 10 / 10
E/Z Centers 2
Optical Activity UNSPECIFIED

Description

E7107 is a semisynthetic derivative of the natural product pladienolide B which was originally isolated from Streptomyces platensis. E7107 is the first compound a new class of anti-cancer agents targeting the spliceosome. Specifically E7107 interacts with the Splicing factor 3B subunit 1 (SF3b1) to block the normal splicing of oncogenes. Development of E7107 was suspended after Phase I clinical trials due to an unacceptable profile of adverse events.

Originator

Approval Year

Targets

Primary TargetPharmacologyConditionPotency

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
Unknown
Primary
Unknown

Cmax

ValueDoseCo-administeredAnalytePopulation
28.5 ng/mL
4 mg/m² single, intravenous
E7107 plasma
Homo sapiens
260 ng/mL
4 mg/m² 1 times / day steady-state, intravenous
E7107 plasma
Homo sapiens

AUC

ValueDoseCo-administeredAnalytePopulation
34.6 ng × h/mL
4 mg/m² single, intravenous
E7107 plasma
Homo sapiens
37.1 ng × h/mL
4 mg/m² 1 times / day steady-state, intravenous
E7107 plasma
Homo sapiens

T1/2

ValueDoseCo-administeredAnalytePopulation
8 h
4 mg/m² single, intravenous
E7107 plasma
Homo sapiens
9.2 h
4 mg/m² 1 times / day steady-state, intravenous
E7107 plasma
Homo sapiens

Doses

AEs

PubMed

Sample Use Guides

In Vivo Use Guide
Human patients with solid tumors were treated at escalating doses beginning at 0.6 mg/m^2. E7107 was received as a 30-minute intravenous infusion on Days 1 and 8 and repeating this cycle every 21 days. Selection of subsequent dose levels was performed according to accelerated design.
Route of Administration: Intravenous
In Vitro Use Guide
Unknown
Substance Class Chemical
Record UNII
R60DZX1E2N
Record Status Validated (UNII)
Record Version