uracil mustard

Small moleculeapproved

Approved

Sep 13, 1962

Uramustine (INN) or uracil mustard is a chemotherapy drug which belongs to the class of alkylating agents. It is used in lymphatic malignancies such as non-Hodgkin's lymphoma. Uracil Mustard selectively inhibits the synthesis of deoxyribonucleic acid (DNA). The guanine and cytosine content correlates with the degree of Uracil Mustard-induced cross-linking. At high concentrations of the drug, cellular RNA and protein synthesis are also suppressed. After activation, it binds preferentially to the guanine and cytosine moieties of DNA, leading to cross-linking of DNA, thus inhibiting DNA synthesis and function. The DNA damage leads to apoptosis of the affected cells. Chemically it is a derivative of nitrogen mustard and uracil. — NCATS

Clinical trial activity

0 trials · 0 clinical orgs · 2 marketing orgs

Phase 1
0
Phase 2
0
Phase 3
0
Phase 4
0

Timeline

1960s

  1. Sep 13, 1962

    Earliest FDA Approval

  2. Sep 13, 1962

    Shire — NDA Secondary Org

Indications

Mechanism of action

  • DNAINHIBITOR

    DNA inhibitor

    Alkylating agent

Approval history

  • approvedPriority reviewSep 13, 1962

Chemistry & pharmacology

Loading structure…

SMILES

ClCCN(CCCl)C1=CNC(=O)NC1=O
Mol. weight
252.098 g/mol
Lipinski Ro5
Pass
Rule of 3
No
Chirality
Achiral Molecule
Inorganic
No
Polymer
No
Delivery
Oral
Availability
Discontinued

Oral

Yes

Parenteral

No

Topical

No

Sources

Also known as

  • 5-aminouracil mustard
  • 5-aminouracil mustard
  • 5-[bis(2-chloroethyl)amino]-2,4(1h,3h)-pyrimidinedione
  • 5-[bis(2-chloroethyl)amino]-2,4(1h,3h)-pyrimidinedione
  • 5-(di-2-chloroethyl)aminouracil
  • 5-(di-2-chloroethyl)aminouracil
  • 5-[di(beta-chloroethyl)amino]uracil
  • 5-[di(beta-chloroethyl)amino]uracil
  • 5-n,n-bis(2-chloroethyl)aminouracil
  • 5-n,n-bis(2-chloroethyl)aminouracil
  • aminouracil mustard
  • aminouracil mustard
  • aminouracil mustard
  • chlorethaminacil
  • demethyldopan
  • desmethyldopan
  • u-8344
  • u-8344
  • uracil mustard
  • uracil mustard
  • uracil mustard
  • uracil mustard
  • uracil mustard
  • uracil mustard
  • uracil mustard
  • uracil mustard
  • uracil mustard
  • uracil mustard
  • uracil mustard
  • uracil nitrogen mustard
  • uracil nitrogen mustard
  • uracil nitrogen mustard
  • uramustin
  • uramustine
  • uramustine
  • uramustine
  • uramustine

Organizations

Marketing (2)

OrganizationOrg typeRelationshipDate
ShireFor profitNDA2Sep 13, 1962
UpjohnFor profitNDA