AFELETECAN

Investigational

Details

Stereochemistry	ABSOLUTE
Molecular Formula	C45H49N7O11S
Molecular Weight	895.976
Optical Activity	UNSPECIFIED
Defined Stereocenters	8 / 8
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

SMILES

CC[C@@]4(OC(=O)[C@@H](NC(=O)[C@H](CC1=CNC=N1)NC(=S)NC2=CC=C(O[C@H]3O[C@@H](C)[C@@H](O)[C@@H](OC)[C@@H]3O)C=C2)C(C)C)C(=O)OCC5=C4C=C6N(CC7=CC8=C(C=CC=C8)N=C67)C5=O

InChI

InChIKey=SLOJCSGNHWIKIG-JNYZSSQASA-N

InChI=1S/C45H49N7O11S/c1-6-45(30-17-33-35-25(15-24-9-7-8-10-31(24)49-35)19-52(33)40(56)29(30)20-60-43(45)58)63-41(57)34(22(2)3)51-39(55)32(16-27-18-46-21-47-27)50-44(64)48-26-11-13-28(14-12-26)62-42-37(54)38(59-5)36(53)23(4)61-42/h7-15,17-18,21-23,32,34,36-38,42,53-54H,6,16,19-20H2,1-5H3,(H,46,47)(H,51,55)(H2,48,50,64)/t23-,32-,34-,36+,37-,38+,42+,45-/m0/s1

HIDE SMILES / InChI

Molecular Formula	C45H49N7O11S
Molecular Weight	895.976
Charge	0
Count	MOL RATIO 1 MOL RATIO (average)

Stereochemistry	ABSOLUTE
Additional Stereochemistry	No
Defined Stereocenters	8 / 8
E/Z Centers	0
Optical Activity	UNSPECIFIED

Description

Afeletecan (Bay 38-3441) is a camptothecin glycoconjugate which stabilizes the active lactone form of camptothecin and allows selective uptake into tumor cells. Afeletecan is a topoisomerase inhibitor. Afeletecan was in phase I clinical trials with Bayer for the treatment of cancer; however, development appears to have been discontinued.

Originator

Approval Year

PubMed

Show entries

Title	Date	PubMed
Gateways to clinical trials.	2003 Jul-Aug	12949633
Gateways to clinical trials. March 2003.	2003 Mar	12731460

Showing 1 to 2 of 2 entries

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Patents

Sample Use Guides

In Vivo Use Guide

Solid tumors: A total of 81 patients with advanced solid tumors were treated with BAY 38-3441 either at doses of 20, 40, 67, 100, 140, 210, 315, 470 and 600 mg/m2/day for 1 day every 3 weeks (single-dose schedule), or at doses of 126, 189, 246, 320 and 416 mg/m2/day once daily for three consecutive days every 3 weeks (3-day schedule). 3-day schedule for BAY 38-3441 at a dose of 320 mg/m2/day as 30-min infusions for further phase II studies was recommended.

Route of Administration: Intravenous