INNO-206

• CAT Number: I001395
• CAS Number: 1361644-26-9
• Molecular Formula: C37H42N4O13
• Molecular Weight: 750.758
• Purity: ≥95%
• Target: ADCs;Topoisomerase
• Solubility: 10 mM in DMSO
• Storage: Store at -20°C
• IUPAC Name: N-[(E)-[1-[(2S,4S)-4-[(2R,4S,5S,6S)-4-amino-5-hydroxy-6-methyloxan-2-yl]oxy-2,5,12-trihydroxy-7-methoxy-6,11-dioxo-3,4-dihydro-1H-tetracen-2-yl]-2-hydroxyethylidene]amino]-6-(2,5-dioxopyrrol-1-yl)hexanamide
• InChI: InChI=1S/C37H42N4O13/c1-17-32(46)20(38)13-27(53-17)54-22-15-37(51,23(16-42)39-40-24(43)9-4-3-5-12-41-25(44)10-11-26(41)45)14-19-29(22)36(50)31-30(34(19)48)33(47)18-7-6-8-21(52-2)28(18)35(31)49/h6-8,10-11,17,20,22,27,32,42,46,48,50-51H,3-5,9,12-16,38H2,1-2H3,(H,40,43)/b39-23+/t17-,20-,22-,27-,32+,37-/m0/s1
• InChIKey: OBMJQRLIQQTJLR-USGQOSEYSA-N
• SMILES: CC1C(C(CC(O1)OC2CC(CC3=C(C4=C(C(=C23)O)C(=O)C5=C(C4=O)C=CC=C5OC)O)(C(=NNC(=O)CCCCCN6C(=O)C=CC6=O)CO)O)N)O

INNO-206(CAT: I001395), also known as aldoxorubicin, is a novel prodrug of the anthracycline chemotherapeutic agent doxorubicin. It is designed to improve the therapeutic index of doxorubicin by selectively delivering it to tumor tissues while minimizing exposure to healthy tissues. INNO-206 utilizes a linker technology that allows for the preferential release of doxorubicin in the tumor microenvironment, potentially reducing systemic toxicity. Preclinical studies have shown that INNO-206 has enhanced antitumor activity compared to doxorubicin in various cancer models. Clinical trials have evaluated its efficacy and safety in several cancer types, including soft tissue sarcoma and advanced pancreatic cancer. Further research is ongoing to explore its potential benefits in cancer treatment.

Overview of Clinical Research

Originator: KTB Tumorforschungs
Developer: CytRx Corporation
Class: Anthracyclines; Cytostatic antibiotics; Doxorubicins; Hydrazines; Maleimides; Pyrroles; Small molecules
Mechanism of Action: DNA intercalators; Reactive oxygen species stimulants; Type II DNA topoisomerase inhibitors
Orphan Drug Status: Yes – Small cell lung cancer; Soft tissue sarcoma; Pancreatic cancer; Glioblastoma; Ovarian cancer
New Molecular Entity: No

Reference

1: Sachdev E, Sachdev D, Mita M. Aldoxorubicin for the treatment of soft tissue sarcoma. Expert Opin Investig Drugs. 2017 Oct;26(10):1175-1179. doi: 10.1080/13543784.2017.1371134. Epub 2017 Aug 28. Review. PubMed PMID: 28846045.
2: Chugh R, Schuetze SM. Aldoxorubicin in Sarcoma: Teaching an Old Drug New Tricks. JAMA Oncol. 2015 Dec;1(9):1280-1. doi: 10.1001/jamaoncol.2015.3221. PubMed PMID: 26379207.
3: Chawla SP, Papai Z, Mukhametshina G, Sankhala K, Vasylyev L, Fedenko A, Khamly K, Ganjoo K, Nagarkar R, Wieland S, Levitt DJ. First-Line Aldoxorubicin vs Doxorubicin in Metastatic or Locally Advanced Unresectable Soft-Tissue Sarcoma: A Phase 2b Randomized Clinical Trial. JAMA Oncol. 2015 Dec;1(9):1272-80. doi: 10.1001/jamaoncol.2015.3101. PubMed PMID: 26378637.
4: Mita MM, Natale RB, Wolin EM, Laabs B, Dinh H, Wieland S, Levitt DJ, Mita AC. Pharmacokinetic study of aldoxorubicin in patients with solid tumors. Invest New Drugs. 2015 Apr;33(2):341-8. doi: 10.1007/s10637-014-0183-5. Epub 2014 Nov 12. PubMed PMID: 25388939; PubMed Central PMCID: PMC4387275.
5: Chawla SP, Chua VS, Hendifar AF, Quon DV, Soman N, Sankhala KK, Wieland DS, Levitt DJ. A phase 1B/2 study of aldoxorubicin in patients with soft tissue sarcoma. Cancer. 2015 Feb 15;121(4):570-9. doi: 10.1002/cncr.29081. Epub 2014 Oct 13. PubMed PMID: 25312684.
6: Marrero L, Wyczechowska D, Musto AE, Wilk A, Vashistha H, Zapata A, Walker C, Velasco-Gonzalez C, Parsons C, Wieland S, Levitt D, Reiss K, Prakash O. Therapeutic efficacy of aldoxorubicin in an intracranial xenograft mouse model of human glioblastoma. Neoplasia. 2014 Oct 23;16(10):874-82. doi: 10.1016/j.neo.2014.08.015. eCollection 2014 Oct. PubMed PMID: 25379024; PubMed Central PMCID: PMC4212249.