Identification

Generic Name
XMT-1001
DrugBank Accession Number
DB06069
Background

XMT-1001 is a polymer-based prodrug of camptothecin (CPT), a well-characterized topoisomerase I inhibitor with potent anti-tumor activity. It is a water-soluble macromolecular conjugate of camptothecin (CPT). In this novel CPT pro-drug, CPT is conjugated with a 70 kDa biodegradable hydrophilic polyacetal, poly (1-hydroxymethylene hydroxylmethylformal). XMT-1001 has demonstrated an improved therapeutic window as compared with CPT and irinotecan in human tumor xenografts models

Type
Small Molecule
Groups
Investigational
Synonyms
Not Available

Pharmacology

Indication

Investigated for use/treatment in solid tumors.

Reduce drug development failure rates
Build, train, & validate machine-learning models
with evidence-based and structured datasets.
See how
Build, train, & validate predictive machine-learning models with structured datasets.
See how
Contraindications & Blackbox Warnings
Avoid life-threatening adverse drug events
Improve clinical decision support with information on contraindications & blackbox warnings, population restrictions, harmful risks, & more.
Learn more
Avoid life-threatening adverse drug events & improve clinical decision support.
Learn more
Pharmacodynamics

In preclinical studies, XMT-1001 was better tolerated and more efficacious than either camptothecin or irinotecan in models of human cancer, showing extended plasma half-life and high concentrations in tumor tissue. The Phase I results show that, in humans, camptothecin, the active agent in XMT-1001, is released gradually from the Fleximer carrier as a pro-drug in a manner that will potentially avoid common safety problems associated with drugs in this class.

Mechanism of action

XMT-1001 is Mersana’s most advanced Fleximer®-based product candidate. It utilizes a novel, dual release mechanism to liberate a camptothecin prodrug, which is then converted within cells into camptothecin, a DNA topoisomerase I inhibitor. It is a potent inhibitor of LS174 and A2780 human tumor xenografts in a mouse model.

TargetActionsOrganism
UDNA topoisomerase 1Not AvailableHumans
Absorption

Not Available

Volume of distribution

Not Available

Protein binding

Not Available

Metabolism
Not Available
Route of elimination

Not Available

Half-life

Not Available

Clearance

Not Available

Adverse Effects
Improve decision support & research outcomes
With structured adverse effects data, including: blackbox warnings, adverse reactions, warning & precautions, & incidence rates.
Learn more
Improve decision support & research outcomes with our structured adverse effects data.
Learn more
Toxicity

Not Available

Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
Not Available
Food Interactions
Not Available

Categories

Drug Categories
Classification
Not classified
Affected organisms
Not Available

Chemical Identifiers

UNII
Not Available
CAS number
Not Available
InChI Key
Not Available
InChI
Not Available
IUPAC Name
Not Available
SMILES
Not Available

References

General References
Not Available
PubChem Substance
347910326

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
1CompletedTreatmentNon-Small Cell Lung Carcinoma (NSCLC) / Small Cell Lung Cancer (SCLC)1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage Forms
Not Available
Prices
Not Available
Patents
Not Available

Properties

State
Solid
Experimental Properties
Not Available
Predicted Properties
Not Available
Predicted ADMET Features
Not Available

Spectra

Mass Spec (NIST)
Not Available
Spectra
Not Available

Targets

Build, predict & validate machine-learning models
Use our structured and evidence-based datasets to unlock new
insights and accelerate drug research.
Learn more
Use our structured and evidence-based datasets to unlock new insights and accelerate drug research.
Learn more
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
General Function
Poly(a) rna binding
Specific Function
Releases the supercoiling and torsional tension of DNA introduced during the DNA replication and transcription by transiently cleaving and rejoining one strand of the DNA duplex. Introduces a singl...
Gene Name
TOP1
Uniprot ID
P11387
Uniprot Name
DNA topoisomerase 1
Molecular Weight
90725.19 Da

Drug created at November 18, 2007 18:29 / Updated at June 12, 2020 16:52