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EC0531

has antineoplastic activity; structure in first source

Networked: 2 relevant articles (0 outcomes, 1 trials/studies)

Bio-Agent Context: Research Results

Heterocyclic Compounds: 198
- Fused-Ring Heterocyclic Compounds
  - 2-Ring Heterocyclic Compounds
    - Pteridines: 147
      - Pterins: 160
        Folic Acid: 19425
        EC0531: 2
Amino Acids, Peptides, and Proteins: 1
- Peptides: 82426
  - Oligopeptides: 519
    - EC0531: 2

Experts

1.	Klein, Patrick J: 2 articles (12/2018 - 06/2017)
2.	Leamon, Christopher P: 2 articles (12/2018 - 06/2017)
3.	Vlahov, Iontcho R: 2 articles (12/2018 - 06/2017)
4.	Cournoyer, Ashleigh M: 1 article (12/2018)
5.	Deshuillers, Pierre L: 1 article (12/2018)
6.	Dhawan, Deepika: 1 article (12/2018)
7.	Fourez, Lindsey M: 1 article (12/2018)
8.	Heng, Hock Gan: 1 article (12/2018)
9.	Knapp, Deborah W: 1 article (12/2018)
10.	Low, Philip S: 1 article (12/2018)

Related Diseases

1.	Neoplasms (Cancer) 12/11/2018 - "A 3+3 dose escalation study of EC0531 (starting dose 0.2 mg/kg given intravenously at two-week intervals) was performed in dogs with iUC expressing high levels of FRs (>50% positive tumor cells). " 06/01/2017 - "Using 3H-labeled compounds, more than a 12-fold higher amount of tubulysin was measured in a FR + human tumor xenograft compared to the unconjugated drug, a finding that explains, in part, why EC0531 displays curative activity, whereas the unconjugated tubulysin agent is essentially inactive. " 06/01/2017 - "EC0531 was found to produce greater FR-specific anti-tumor activity at lower dose levels than EC0305; furthermore, EC0531's maximum tolerated dose level was significantly higher than that of EC0305, likely because EC0531's saccharopeptidic-based spacer allows for ~sixfold reduction in hepatic clearance. " 06/01/2017 - "Human tumor xenografts were used to directly compare EC0305 and EC0531's antitumor activity. "
2.	Neutropenia 12/11/2018 - "Unlike human neutrophils, canine neutrophils were found to express FRs, which contributes to the neutropenia at higher doses of EC0531 in dogs. " 12/11/2018 - "The MTD of EC0531 was 0.26 mg/kg every two weeks, with grade 3-4 neutropenia and gastrointestinal toxicity observed at higher doses. "
3.	Carcinoma (Carcinomatosis) 12/11/2018 - "The purpose was to determine the safety and antitumor activity of a folate-tubulysin conjugate (EC0531) in a relevant preclinical animal model, dogs with naturally-occurring invasive urothelial carcinoma (iUC). "

Related Drugs and Biologics

1.	Folic Acid (Vitamin M)
2.	EC0305