Monoclonal antibody | |
---|---|
Type | Whole antibody |
Source | Humanized |
Target | DLL3 |
Clinical data | |
ATC code |
|
Identifiers | |
CAS Number | |
ChemSpider |
|
UNII | |
KEGG | |
Chemical and physical data | |
Formula | C6416H9894N1698O2028S46 (non- glycosylated) |
Rovalpituzumab tesirine (Rova-T) is an experimental antibody-drug conjugate targeting the protein DLL3 on tumor cells. [1] [2] It was originally developed by Stemcentrx and was purchased by AbbVie. [3] It was tested for use in small-cell lung cancer, but development was terminated after unsuccessful phase III trial. [4] [5]
In 2018, an Independent Data Monitoring Committee found that in the TAHOE phase III trial, Rova-T shortened survival of lung cancer patients compared to SOC chemotherapy topotecan, prompting termination of trial enrollment. Another phase III trial (MERU) demonstrated no survival benefit over placebo. [6] [7] A phase II trial using the drug as a third-line treatment for relapsed or refractory lung cancer showed objective response rate at just 16%. [8]
Chemical structure of "tesirine" (drawn in black). It consists of a pyrrolobenzodiazepine type dimer (top), which is the actual anti-cancer agent, a Val– Ala structure that can be cleaved by an enzyme to detach the anti-cancer agent from the antibody, a polyethylene glycol spacer, and a maleimide linker which is attached to a cysteine in the antibody's (rovalpituzumab's) peptide backbone, drawn blue. Each rovalpituzumab molecule has an average of two such attachments. [9]
{{
cite web}}
: CS1 maint: multiple names: authors list (
link) CS1 maint: numeric names: authors list (
link)
Monoclonal antibody | |
---|---|
Type | Whole antibody |
Source | Humanized |
Target | DLL3 |
Clinical data | |
ATC code |
|
Identifiers | |
CAS Number | |
ChemSpider |
|
UNII | |
KEGG | |
Chemical and physical data | |
Formula | C6416H9894N1698O2028S46 (non- glycosylated) |
Rovalpituzumab tesirine (Rova-T) is an experimental antibody-drug conjugate targeting the protein DLL3 on tumor cells. [1] [2] It was originally developed by Stemcentrx and was purchased by AbbVie. [3] It was tested for use in small-cell lung cancer, but development was terminated after unsuccessful phase III trial. [4] [5]
In 2018, an Independent Data Monitoring Committee found that in the TAHOE phase III trial, Rova-T shortened survival of lung cancer patients compared to SOC chemotherapy topotecan, prompting termination of trial enrollment. Another phase III trial (MERU) demonstrated no survival benefit over placebo. [6] [7] A phase II trial using the drug as a third-line treatment for relapsed or refractory lung cancer showed objective response rate at just 16%. [8]
Chemical structure of "tesirine" (drawn in black). It consists of a pyrrolobenzodiazepine type dimer (top), which is the actual anti-cancer agent, a Val– Ala structure that can be cleaved by an enzyme to detach the anti-cancer agent from the antibody, a polyethylene glycol spacer, and a maleimide linker which is attached to a cysteine in the antibody's (rovalpituzumab's) peptide backbone, drawn blue. Each rovalpituzumab molecule has an average of two such attachments. [9]
{{
cite web}}
: CS1 maint: multiple names: authors list (
link) CS1 maint: numeric names: authors list (
link)