Estramustine

Estramustine Brand Name– Emcyt

What is Estramustine

Estramustine is an oral, nitrogen mustard antineoplastic agent that is used to treat prostate cancer.

Estramustine is a combination of an estradiol molecule linked to nornitrogen mustard.

The oral compound contains a phosphate group that facilitates higher water solubility and oral absorption. In patients with hormone-refractory prostate cancer, estramustine has produced responses in 30—60% of patients as measured by reductions in tumor size, pain, and prostate specific antigen levels.

Combination therapy of estramustine with paclitaxel, etoposide, or vinorelbine for the treatment of prostate or breast cancers is being investigated.

Estramustine has also been studied in vitro and in vivo for the treatment of malignant glioma.

The oral form of estramustine phosphate is the disodium salt of the compound.

Estramustine was approved by the FDA in December 21, 1981.

An intravenous formulation of estramustine is under investigation.

Indications

  • prostate cancer

For the treatment of metastatic prostate cancer

for the treatment of hormone-refractory, metastatic prostate cancer in combination with docetaxel

Side Effects

  1. angioedema
  2. anorexia
  3. anxiety
  4. chest pain (unspecified)
  5. diarrhea
  6. dyspepsia
  7. dyspnea
  8. ecchymosis
  9. edema
  10. elevated hepatic enzymes
  11. emotional lability
  12. flatulence
  13. fluid retention
  14. flushing
  15. GI bleeding
  16. gynecomastia
  17. gynecomastia
  18. headache
  19. heart failure
  20. hoarseness
  21. hyperbilirubinemia
  22. impotence (erectile dysfunction)
  23. insomnia
  24. lacrimation
  25. lethargy
  26. leukopenia
  27. mastalgia
  28. muscle cramps
  29. myocardial infarction
  30. nausea
  31. peripheral edema
  32. phlebitis
  33. polydipsia
  34. pruritus
  35. pulmonary embolism
  36. rash
  37. stroke
  38. thrombocytopenia
  39. thromboembolism
  40. thrombosis
  41. vomiting
  42. xerosis

Monitoring Parameters

  • CBC with differential
  • LFTs
  • serum creatinine/BUN

Contraindications

  • breast-feeding
  • cardiac disease
  • cerebrovascular disease
  • children
  • coronary artery disease
  • diabetes mellitus
  • heart failure
  • hepatic disease
  • herpes infection
  • hypercalcemia
  • hypertension
  • hypocalcemia
  • jaundice
  • male-mediated teratogenicity
  • migraine
  • myocardial infarction
  • peripheral edema
  • pregnancy
  • renal failure
  • renal impairment
  • seizure disorder
  • stroke
  • thromboembolic disease
  • thrombophlebitis
  • vaccination
  • varicella
  • viral infection

Interactions

  • Abciximab
  • Acarbose
  • Acetohexamide
  • Alogliptin; Metformin
  • Alogliptin; Pioglitazone
  • Alpha interferons
  • Alpha-glucosidase Inhibitors
  • Alteplase
  • Anagrelide
  • Anticoagulants
  • Antithrombin III
  • Antithymocyte Globulin
  • Apixaban
  • Argatroban
  • Aspirin, ASA; Dipyridamole
  • Azelastine; Fluticasone
  • Bacillus Calmette-Guerin Vaccine, BCG
  • Beclomethasone
  • Betamethasone
  • Betrixaban
  • Bivalirudin
  • Budesonide
  • Budesonide; Formoterol
  • Calcium
  • Canagliflozin; Metformin
  • Carbamazepine
  • Chlorpropamide
  • Ciclesonide
  • Cilostazol
  • Clobazam
  • Clopidogrel
  • Clozapine
  • Corticosteroids
  • Cortisone
  • Dabigatran
  • Dalteparin
  • Danaparoid
  • Dapagliflozin; Metformin
  • Deflazacort
  • Desirudin
  • Dexamethasone
  • Diclofenac
  • Diclofenac; Misoprostol
  • Digoxin
  • Diphenhydramine; Ibuprofen
  • Diphenhydramine; Naproxen
  • Dipyridamole
  • Echinacea
  • Edoxaban
  • Empagliflozin; Linagliptin; Metformin
  • Empagliflozin; Metformin
  • Enoxaparin
  • Eptifibatide
  • Ertugliflozin; Metformin
  • Esomeprazole; Naproxen
  • Ethotoin
  • Etodolac
  • Famotidine; Ibuprofen
  • Febuxostat
  • Fenoprofen
  • Filgrastim, G-CSF
  • Fludrocortisone
  • Flunisolide
  • Flurbiprofen
  • Fluticasone
  • Fluticasone; Salmeterol
  • Fluticasone; Umeclidinium; Vilanterol
  • Fluticasone; Vilanterol
  • Fondaparinux
  • food
  • Formoterol; Mometasone
  • Fosphenytoin
  • Glimepiride
  • Glimepiride; Pioglitazone
  • Glimepiride; Rosiglitazone
  • Glipizide
  • Glipizide; Metformin
  • Glyburide
  • Glyburide; Metformin
  • Heparin
  • Hydantoins
  • Hydrocodone; Ibuprofen
  • Hydrocortisone
  • Ibuprofen
  • Ibuprofen; Oxycodone
  • Ibuprofen; Pseudoephedrine
  • Indomethacin
  • Influenza Virus Vaccine
  • Insulins
  • Interferon Alfa-2a
  • Interferon Alfa-2b
  • Interferon Alfa-2b; Ribavirin
  • Interferon Alfa-n3
  • Interferon Alfacon-1
  • Intranasal Influenza Vaccine
  • Ketoprofen
  • Ketorolac
  • Lansoprazole; Naproxen
  • Lepirudin
  • Linagliptin; Metformin
  • Live Vaccines
  • Measles Virus; Mumps Virus; Rubella Virus; Varicella Virus Vaccine, Live
  • Measles/Mumps/Rubella Vaccines, MMR
  • Meclofenamate Sodium
  • Mefenamic Acid
  • Meglitinides
  • Meloxicam
  • Metformin
  • Metformin; Pioglitazone
  • Metformin; Repaglinide
  • Metformin; Rosiglitazone
  • Metformin; Saxagliptin
  • Metformin; Sitagliptin
  • Methylprednisolone
  • Miglitol
  • Mometasone
  • Nabumetone
  • Naproxen
  • Naproxen; Pseudoephedrine
  • Naproxen; Sumatriptan
  • Nateglinide
  • Nefazodone
  • Oxaprozin
  • Palifermin
  • Peginterferon Alfa-2a
  • Peginterferon Alfa-2b
  • Penicillamine
  • Pentosan
  • Phenytoin
  • Pioglitazone
  • Piroxicam
  • Platelet Inhibitors
  • Polycarbophil
  • Prasugrel
  • Prednisolone
  • Prednisone
  • Repaglinide
  • Reteplase, r-PA
  • Rivaroxaban
  • Rosiglitazone
  • Rotavirus Vaccine
  • Rubella Virus Vaccine Live
  • Smallpox and Monkeypox Vaccine, Live, Nonreplicating
  • Smallpox Vaccine, Vaccinia Vaccine
  • Streptokinase
  • Sulfonylureas
  • Sulindac
  • Tbo-Filgrastim
  • Tenecteplase
  • Thiazolidinediones
  • Thrombolytic Agents
  • Ticagrelor
  • Ticlopidine
  • Tinzaparin
  • Tirofiban
  • Tolazamide
  • Tolbutamide
  • Tolmetin
  • Triamcinolone
  • Tuberculin Purified Protein Derivative, PPD
  • Typhoid Vaccine
  • Urokinase
  • Varicella-Zoster Virus Vaccine, Live
  • Vorapaxar
  • Warfarin
  • Yellow Fever Vaccine, Live
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