bexarotene (targretin) Report issue

Small molecule Orphan Drug FDA Approved FDA Priority Review FDA
AACT ChEMBL DrugBank Drug Central Drugs@FDA KEGG MeSH PubChem repoDB

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Bexarotene (Targretin) is an antineoplastic agent indicated by the FDA for Cutaneous T cell lymphoma. It has been used off-label for lung cancer, breast cancer, and Kaposi's sarcoma. Bexarotene is a member of a subclass of retinoids that selectively activate retinoid X receptors (RXRs). These retinoid receptors have biologic activity distinct from that of retinoic acid receptors (RARs). Bexarotene selectively binds and activates retinoid X receptor subtypes (RXRa, RXRb, RXRg). RXRs can form heterodimers with various receptor partners such as retinoic acid receptors (RARs), vitamin D receptor, thyroid receptor, and peroxisome proliferator activator receptors (PPARs). Once activated, these receptors function as transcription factors that regulate the expression of genes that control cellular differentiation and proliferation. Bexarotene inhibits the growth in vitro of some tumor cell lines of hematopoietic and squamous cell origin. It also induces tumor regression in vivo in some animal models. The exact mechanism of action of bexarotene in the treatment of cutaneous T-cell lymphoma (CTCL) is unknown.   NCATS

Chemistry

  • SMILES: CC1=C(C=C2C(=C1)C(C)(C)CCC2(C)C)C(=C)C3=CC=C(C=C3)C(O)=O
  • InChIKey: NAVMQTYZDKMPEU-UHFFFAOYSA-N
  • Mol. Mass: 348.4779
  • ALogP: 6.1
  • ChEMBL Molecule:
    bexarotene  
More Chemistry

Pharmacology

Drug Pricing (per unit)

United States

$12.0000 - $317.4772
More Pricing Detail

Note: This drug pricing data is preliminary, incomplete, and may contain errors.

Alternative names

3-methyl-ttneb | 4-(1-(3,5,5,8,8-pentamethyl-5,6,7,8-tetrahydro-2-naphthyl)ethenyl)benzoic acid | 4-[1-(3,5,5,8,8-pentamethyltetralin-2-yl)ethenyl]benzoic acid | 4-[1-(5,6,7,8,-tetrahydro-3,5,5,8,8-pentamethyl-2-naphtalenyl)ethenyl]benzoic acid | bexaroten | bexarotene | bexarotène | bexaroteno | bexarotenum | elan brand of bexarotene | lg100069 | lg-100069 | lg69 compound | lgd1069 | lgd 1069 | lgd-1069 | ligand brand of bexarotene | p-(1-(5,6,7,8-tetrahydro-3,5,5,8,8-pentamethyl-2-naphthyl)vinyl)benzoic acid | p-[1-(5,6,7,8,-tetrahydro-3,5,5,8,8-pentamethyl-2-naphthyl)vinyl]benzoic acid | targretin | targretine | targretyn | targrexin

Organizations (56)

Research & Development (49)

Organization Org Type FDA approvals Clinical Trials involvement Org ID Force Sort

Marketing (9)

Organization Org Type FDA approvals Clinical Trials involvement Org ID Force Sort

Indications (28)

Approved Indications (2)


 

Lymphoma, T-Cell

Lymphoma, T-Cell, Cutaneous

Experimental Indications - Clinical Trial Phases 1-4 (28)


 

Alopecia Areata (Phase 2/Phase 3)

Alzheimer Disease (Phase 2)

Breast Neoplasms (Phase 2)

Carcinoma, Non-Small-Cell Lung (Phase 3)

Cognition (Phase 3)

HIV Infections (Phase 2)

Hyperplasia (Phase 1)

Leukemia (Phase 2)

Leukemia, Myeloid, Acute (Phase 2)

Lung Neoplasms (Phase 2)

Lymphoma (Phase 3)

Lymphoma, Primary Cutaneous Anaplastic Large Cell (Phase 3)

Lymphoma, T-Cell (Phase 4)

Lymphoma, T-Cell, Cutaneous ()

Multiple Myeloma (Phase 1)

Mycosis Fungoides (Phase 3)

Myelodysplastic-Myeloproliferative Diseases (Phase 2)

Myelodysplastic Syndromes (Phase 2)

Neoplasms ()

Parapsoriasis (Phase 2)

Pituitary ACTH Hypersecretion (Phase 1/Phase 2)

Psoriasis (Phase 2)

Psychotic Disorders (Phase 3)

Sarcoma, Kaposi (Phase 2)

Schizophrenia (Phase 3)

Sezary Syndrome (Phase 2)

Squamous Cell Carcinoma of Head and Neck (Phase 1)

Thyroid Neoplasms (Early Phase 1)

Overview

  • Highest Phase: Phase 4
  • # of Trials: 44
  • # of Trial Organizations: 49

Trials by Phase

Trial Phase Start Date Organizations Indications

Feedback

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