Vorinostat
Vorinostat Uses, Dosage, Side Effects, Food Interaction and all others data.
Vorinostat (rINN) or suberoylanilide hydroxamic acid (SAHA), is a drug currently under investigation for the treatment of cutaneous T cell lymphoma (CTCL), a type of skin cancer, to be used when the disease persists, gets worse, or comes back during or after treatment with other medicines. It is the first in a new class of agents known as histone deacetylase inhibitors. A recent study suggested that vorinostat also possesses some activity against recurrent glioblastoma multiforme, resulting in a median overall survival of 5.7 months (compared to 4 - 4.4 months in earlier studies). Further brain tumor trials are planned using combinations of vorinostat with other drugs.
| Trade Name | Vorinostat |
| Availability | Prescription only |
| Generic | Vorinostat |
| Vorinostat Other Names | Octanedioic acid hydroxyamide phenylamide, SAHA, Suberanilohydroxamic acid, Suberoylanilide hydroxamic acid, Vorinostat, Vorinostatum |
| Related Drugs | bexarotene, methoxsalen, Targretin, romidepsin, Targretin Gel |
| Weight | 100mg |
| Type | Oral capsule |
| Formula | C14H20N2O3 |
| Weight | Average: 264.3202 Monoisotopic: 264.147392516 |
| Protein binding | 71% |
| Groups | Approved, Investigational |
| Therapeutic Class | |
| Manufacturer | |
| Available Country | United States |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
Vorinostat is a histone deacetylase (HDAC) inhibitor used for the treatment of cutaneous manifestations in patients with progressive, persistent, or recurrent cutaneous T- cell lymphoma (CTCL) following prior systemic therapies.
For the treatment of cutaneous manifestations in patients with cutaneous T-cell lymphoma who have progressive, persistent or recurrent disease on or following two systemic therapies.
Vorinostat is also used to associated treatment for these conditions: Persistent Cutaneous T-Cell Lymphoma, Progressive Cutaneous T-cell lymphoma, Recurrent Cutaneous T-cell lymphoma
How Vorinostat works
Vorinostat inhibits the enzymatic activity of histone deacetylases HDAC1, HDAC2 and HDAC3 (Class I) and HDAC6 (Class II) at nanomolar concentrations (IC50< 86 nM). These enzymes catalyze the removal of acetyl groups from the lysine residues of histones proteins. In some cancer cells, there is an overexpression of HDACs, or an aberrant recruitment of HDACs to oncogenic transcription factors causing hypoacetylation of core nucleosomal histones. By inhibiting histone deacetylase, vorinostat causes the accumulation of acetylated histones and induces cell cycle arrest and/or apoptosis of some transformed cells. The mechanism of the antineoplastic effect of vorinostat has not been fully characterized.
Food Interaction
- Take with food.
Vorinostat Drug Interaction
Unknown: everolimus, contained in alcoholic beverages , sulfamethoxazole / trimethoprim, aspirin, prochlorperazine, dexamethasone, fentanyl, cyclobenzaprine, bismuth subsalicylate, levetiracetam, potassium chloride, levofloxacin, lidocaine topical, enoxaparin, psyllium, morphine, morphine, bismuth subsalicylate, acetaminophen / oxycodone, potassium phosphate / sodium phosphate
Vorinostat Disease Interaction
Major: thromboembolismModerate: diabetes, GI disturbances, liver impairment, myelosuppression
Half Life
2 hours
Elimination Route
In vitro studies using human liver microsomes indicate negligible biotransformation by cytochromes P450 (CYP). Vorinostat is eliminated predominantly through metabolism with less than 1% of the dose recovered as unchanged drug in urine, indicating that renal excretion does not play a role in the elimination of vorinostat. However, renal excretion does not play a role in the elimination of vorinostat.
Innovators Monograph
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