Ledertepa Uses, Dosage, Side Effects and more
N,N'N'-triethylenethiophosphoramide (ThioTEPA) is a cancer chemotherapeutic member of the alkylating agent group, now in use for over 50 years. It is a stable derivative of N,N',N''- triethylenephosphoramide (TEPA). It is mostly used to treat breast cancer, ovarian cancer and bladder cancer. It is also used as conditioning for Bone marrow transplantation. Its main toxicity is myelosuppression.
The unstable nitrogen-carbon groups alkylate with DNA causing irrepairable DNA damage. They stop tumor growth by crosslinking guanine nucleobases in DNA double-helix strands, directly attacking DNA. This makes the strands unable to uncoil and separate. As this is necessary in DNA replication, the cells can no longer divide. These drugs act nonspecifically.
| Trade Name | Ledertepa |
| Availability | Prescription only |
| Generic | Thiotepa |
| Thiotepa Other Names | Thiotepa |
| Related Drugs | prednisone, methotrexate, dexamethasone, Arimidex, carboplatin, fluorouracil, doxorubicin, cisplatin, paclitaxel, cyclophosphamide |
| Type | |
| Formula | C6H12N3PS |
| Weight | Average: 189.218 Monoisotopic: 189.048954601 |
| Groups | Approved, Investigational |
| Therapeutic Class | |
| Manufacturer | |
| Available Country | Netherlands |
| Last Updated: | January 7, 2025 at 1:49 am |
Uses
Ledertepa is an alkylating agent used to prevent graft rejection in stem cell transplantation and to treat a variety of malignancies including certain types of adenocarcinoma and superficial bladder carcinomas.
ThioTEPA is used a as conditioning treatment prior to allogeneic or autologous haematopoietic progenitor cell transplantation (HPCT) in haematological diseases in adult and paediatric patients. Also, when high dose chemotherapy with HPCT support it is appropriate for the treatment of solid tumours in adult and paediatric patients.
Ledertepa is also used to associated treatment for these conditions: Adenocarcinoma of the Ovaries, Breast Adenocarcinoma, Papillary transitional cell carcinoma of bladder, Malignant effusion
How Ledertepa works
The alkyl group is attached to the guanine base of DNA, at the number 7 nitrogen atom of the imidazole ring. They stop tumor growth by crosslinking guanine nucleobases in DNA double-helix strands, directly attacking DNA. This makes the strands unable to uncoil and separate. As this is necessary in DNA replication, the cells can no longer divide. These drugs act nonspecifically.
Food Interaction
- Exercise caution with grapefruit products. Grapefruit inhibits the CYP3A4 metabolism of thiotepa, which may increase its serum concentration.
- Exercise caution with St. John's Wort. This herb induces CYP3A4 metabolism and may reduce serum levels of thiotepa.
Ledertepa Drug Interaction
Major: cyclophosphamideModerate: alemtuzumab, cytarabine, oxaliplatin, fludarabineUnknown: encorafenib, calcium / vitamin d, sulfamethoxazole / trimethoprim, ubiquinone, copper gluconate, dexamethasone, meperidine, epoetin alfa, cetuximab, ethanol, metronidazole, glycerin, heparin, ibrutinib, tramadol
Ledertepa Disease Interaction
Major: infections, hepatic dysfunction, myelosuppression, renal dysfunction
Half Life
1.5 to 4.1 hours
Clearance
- 446 +/- 63 mL/min [female patients (45 to 84 years) with advanced stage ovarian cancer receiving 60 mg and 80 mg thiotepa by intravenous infusion on subsequent courses given at 4-week intervals]
Elimination Route
Urinary excretion of 14C-labeled thiotepa and metabolites in a 34-year old patient with metastatic carcinoma of the cecum who received a dose of 0.3 mg/kg intravenously was 63%.
