Tazarotene

Summary

Tazarotene (CHEMBL1657) is an approved small-molecule keratolytic drug (ATC D05AX05) targeting RARA, RARB, and RARG; indicated across 9 conditions including acne and psoriasis.

At a glance

• Status: Approved (max clinical phase 4)
• Modality: Small molecule
• ATC class: D05AX05
• Targets: 3 (RARA, RARB, RARG)
• Indications: 9 conditions
• Clinical trials: 31
• Chemistry: 351.5 Da · C21H21NO2S

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL1657
Name	Tazarotene
Type	Small molecule
Max phase	4
FDA approved	yes
PubChem CID	5381
ChEBI	CHEBI:32184
ATC	D05AX05
Molecular formula	C21H21NO2S
Molecular weight	351.5
InChIKey	OGQICQVSFDPSEI-UHFFFAOYSA-N

SMILES: CCOC(=O)C1=CN=C(C=C1)C#CC2=CC3=C(C=C2)SCCC3(C)C

IUPAC name: ethyl 6-[2-(4,4-dimethyl-2,3-dihydrothiochromen-6-yl)ethynyl]pyridine-3-carboxylate

ChEBI definition: The ethyl ester of tazarotenic acid. A prodrug for tazarotenic acid, it is used for the treatment of psoriasis, acne, and sun-damaged skin.

Pharmacological roles (ChEBI): keratolytic drug, prodrug, teratogenic agent.

Also known as: AGN 190168, AGN-190168, AGN190168, Arazlo, Avage, Fabior, Idp-123, Tazarotene, Tazarotene component of duobrii, Tazarotene component of idp-118, Tazaroteno, Tazorac

Patent coverage: 6,498 distinct patent families (26,405 SureChEMBL compound mentions), from 3 matched compound structure(s). One matched structure accounts for 26,209 (99%) of the total. Mentions count patents naming the compound (not distinct inventions), so promiscuous / reference molecules inflate the mention figure — families are the dedup metric.

Targets

Targets

Primary targets (GtoPdb curated mechanism): the Cancer dependency column is the DepMap CRISPR fitness signal (% of screened cell lines dependent on the target).

Gene	Target	Action	pAffinity	Cancer dependency	UniProt
RARA	Retinoic acid receptor-α	Agonist	7.2	0.8%	P10276
RARB	Retinoic acid receptor-β	Agonist	9.1	0.1%	P10826
RARG	Retinoic acid receptor-γ	Agonist	7.4	1.6%	P13631

Broader ChEMBL bioactivity targets: 5 (assay-derived). Sample: Histone-lysine N-methyltransferase 2A, Retinoic acid receptor gamma, Retinoic acid receptor beta, Retinoic acid receptor alpha, Cytochrome P450 3A4.

Bioactivity

ChEMBL activities: 7 potent at pChembl ≥ 5 of 8 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

Target	pChembl	Type	Value	Unit	Activity ID
RARB	9.1	EC50	0.8	nM	CHEMBL_ACT_2599967
RARB	9.1	EC50	0.8	nM	CHEMBL_ACT_26335877
RARG	7.4	EC50	40	nM	CHEMBL_ACT_2616028
RARG	7.4	EC50	40	nM	CHEMBL_ACT_26335878
RARA	7.2	EC50	63	nM	CHEMBL_ACT_2599947
RARA	7.2	EC50	63	nM	CHEMBL_ACT_26335876
CYP3A4	5.5	IC50	3150	nM	CHEMBL_ACT_27630194

Target pathways

Aggregated over 3 target gene(s): RARA, RARB, RARG.

Top Reactome pathways

6 total, by targets touching each:

Pathway	Targets	Genes
Nuclear Receptor transcription pathway	3	RARA, RARB, RARG
Signaling by Retinoic Acid	3	RARA, RARB, RARG
Activation of anterior HOX genes in hindbrain development during early embryogenesis	3	RARA, RARB, RARG
SUMOylation of intracellular receptors	1	RARA
Transcriptional regulation of granulopoiesis	1	RARA
TGFBR3 expression	1	RARA

Dominant GO biological processes

GO term	Targets
negative regulation of transcription by RNA polymerase II	3
glandular epithelial cell development	3
growth plate cartilage development	3
cell differentiation	3
regulation of myelination	3
multicellular organism growth	3
positive regulation of transcription by RNA polymerase II	3
retinoic acid receptor signaling pathway	3
negative regulation of cartilage development	3
regulation of DNA-templated transcription	3
bone development	3
ureteric bud development	2
neural tube closure	2
outflow tract septum morphogenesis	2
positive regulation of cell population proliferation	2

Indications & clinical

Indications

9 indications (5 at ChEMBL trial phase 4). Phase below is the highest clinical-trial phase recorded for this drug against each disease — not the molecule’s overall approval status (that is in the Summary).

Indication	Trial phase	MONDO	EFO
acne	4	MONDO:0011438	EFO:0003894
psoriasis	4	MONDO:0005083	EFO:0000676
hypopigmentation of the skin	4	MONDO:0019290	Orphanet:183469
lentigo	4	MONDO:0021582	MONDO:0021582
skin disorder	2	MONDO:0005093	EFO:0000701
skin carcinoma	2	MONDO:0002656	EFO:0009259
idiopathic pulmonary fibrosis	2	MONDO:0800504	EFO:0000768
primary cutaneous T-cell non-Hodgkin lymphoma	1	MONDO:0000607	EFO:0002913

1 further indication record had no mapped disease name (EFO/MeSH-only) or were duplicates, and are omitted.

Clinical trials

Total trials: 31.

Phase distribution

Phase	Trials
PHASE2	11
PHASE4	5
PHASE3	5
PHASE1	5
Not specified	4
PHASE1/PHASE2	1

Top trials by phase / activity

NCT	Phase	Status	Title
NCT00648986	PHASE4	COMPLETED	Efficacy and Safety Study of Tazarotene (Tazorac) for the Treatment of Brittle Nails
NCT00834210	PHASE4	COMPLETED	Dapsone Gel 5% and Tazarotene Cream 0.1% Versus Tazarotene Cream 0.1% Monotherapy for Facial Acne Vulgaris
NCT02721173	PHASE4	COMPLETED	Tazarotene Plus Clindamycin vs. Adapalene Plus Clindamycin in the Treatment of Facial Acne Vulgaris
NCT05704114	PHASE4	COMPLETED	Tazarotene 0.045% Lotion for Treating PIE and PIH in Subjects With Acne
NCT06042647	PHASE4	COMPLETED	Anti-Inflammatory Effects of 0.045% Tazarotene/0.01% Halobetasol Lotion in Psoriasis
NCT01017120	PHASE3	COMPLETED	A Study to Evaluate the Safety and Efficacy of Tazarotene Foam, 0.1%, in Subjects With Common Facial Acne
NCT01017146	PHASE3	COMPLETED	A Study to Evaluate the Safety and Efficacy of Tazarotene Foam, 0.1%, in Subjects With Common Facial Acne - W0260-301
NCT02267746	PHASE3	COMPLETED	A Study To Evaluate The Safety And Therapeutic Equivalence of Tazarotene Foam 0.1% in Subjects With Acne Vulgaris
NCT03168321	PHASE3	COMPLETED	A Phase 3, Vehicle-controlled Efficacy and Safety Study of IDP-123 Lotion in the Treatment of Acne Vulgaris (301)
NCT03168334	PHASE3	COMPLETED	A Phase 3, Vehicle-controlled Efficacy and Safety Study of IDP-123 Lotion in the Treatment of Acne Vulgaris (302)
NCT00489086	PHASE2	COMPLETED	Topical Tazarotene in Treating Patients With Basal Cell Skin Cancer and Basal Cell Nevus Syndrome on the Face
NCT00667589	PHASE2	TERMINATED	Sorafenib-induced Hand- Foot Skin Reaction Treatment
NCT00713609	PHASE2	COMPLETED	Safety and Efficacy Study of Clindamycin/Benzoyl Peroxide/Tazarotene Cream in Subjects With Acne
NCT00779896	PHASE1/PHASE2	UNKNOWN	Tazarotene 0.1% Cream For the Treatment of Cutaneous T-Cell Lymphoma: A Prospective Study
NCT00783965	PHASE2	COMPLETED	Topical Tazarotene in Treating Patients With Basal Cell Skin Cancer and Basal Cell Nevus Syndrome on the Chest and Back
NCT01616654	PHASE2	COMPLETED	Dose Range Study of CD5789 in Acne Vulgaris
NCT02525822	PHASE2	UNKNOWN	Study to Compare the Safety and Efficacy of IDP-123 Lotion to Tazorac Cream in the Treatment of Acne Vulgaris
NCT02785159	PHASE2	COMPLETED	Safety and Efficacy of IDP-118 Lotion in the Treatment of Plaque Psoriasis
NCT02938494	PHASE2	COMPLETED	Safety and Efficacy of IDP-123 Lotion to Tazorac® Cream, in the Treatment of Acne Vulgaris
NCT04071756	PHASE2	TERMINATED	Topical Tazarotene Vs Placebo In Hand-Foot-Skin Reactions
NCT05314127	PHASE2	UNKNOWN	Efficacy of Tazarotene in Treatment of Verruca Plana
NCT06331624	PHASE2	COMPLETED	Biomarker Modulation and the Inhibition of NKT1 Cells by Oral GRI-0621 in Patients With IPF
NCT01019603	PHASE1	COMPLETED	A Study to Evaluate the Bioavailability of Tazarotene Foam, 0.1%, and Tazorac Gel, 0.1%, in Subjects With Acne Vulgaris
NCT01112787	PHASE1	COMPLETED	A Study to Evaluate the Irritation Potential of Tazarotene Foam on Skin in Healthy Volunteers
NCT01114841	PHASE1	COMPLETED	A Study To Evaluate The Contact Sensitization Potential Of Tazarotene Foam On Skin In Healthy Volunteers
NCT02849873	PHASE1	COMPLETED	Absorption and Systematic Pharmacokinetics of IDP-123 Lotion in Comparison With Tazorac Cream
NCT03058744	PHASE1	COMPLETED	Topically Applied IDP-118 Lotion and HP Monad Lotion in Subjects With Moderate to Severe Plaque Psoriasis
NCT00440024	Not specified	COMPLETED	The Effect Of A Controlled Daily Skin Care Regimen On Retinoic Acid Tolerance
NCT01053000	Not specified	COMPLETED	Photodynamic Therapy With Levulan® +/- Topical Retinoid Pre-Treatment In The Treatment Of Actinic Keratoses
NCT01094717	Not specified	TERMINATED	Acitretin or Tazarotene Gel and Excimer Laser for Treatment of Psoriasis
NCT06015152	Not specified	COMPLETED	Comparison Of Efficacy Of Tazarotene 0.045% Vs Halobetasol Propionate 0.01% Lotion For Treatment of Scalp Psoriasis

Clinical evidence (CIViC)

No CIViC predictive evidence (expected for non-precision-medicine drugs).

Pharmacology

Pharmacogenomics

No CPIC/DPWG dosing guideline or drug-level clinical/variant annotations in PharmGKB for this molecule.

Related molecules

Related molecules

Molecules sharing ≥1 of this drug’s curated primary targets, merged from two biobtree sources and ranked by shared-target count, then clinical phase: ChEMBL clinical-stage candidates (development phase ≥2) and PubChem drug-class bioactivity (approved / known drugs acting on the target). Deduplicated by drug name; the drug’s own salt forms are excluded. Note: for a drug with few primary targets a shared-target match can reflect off-target / promiscuous binding rather than the same therapeutic mechanism — the phase ordering surfaces bona-fide therapeutics first.

42 molecules share ≥1 primary target. Top 42 by shared-target count:

Molecule	Source	Status	Shared targets
Acetaminophen	ChEMBL + PubChem	Phase 4 (approved)	RARA, RARB, RARG
ADAPALENE	ChEMBL + PubChem	Phase 4 (approved)	RARA, RARB, RARG
ALITRETINOIN	ChEMBL + PubChem	Phase 4 (approved)	RARA, RARB, RARG
Alprostadil	ChEMBL + PubChem	Phase 4 (approved)	RARA, RARB, RARG
Amoxicillin	ChEMBL + PubChem	Phase 4 (approved)	RARA, RARB, RARG
BEXAROTENE	ChEMBL + PubChem	Phase 4 (approved)	RARA, RARB, RARG
cyclosporine	ChEMBL + PubChem	Phase 4 (approved)	RARA, RARB, RARG
Olanzapine	ChEMBL + PubChem	Phase 4 (approved)	RARA, RARB, RARG
REGORAFENIB	ChEMBL + PubChem	Phase 4 (approved)	RARA, RARB, RARG
Rosiglitazone	ChEMBL + PubChem	Phase 4 (approved)	RARA, RARB, RARG
Tolcapone	ChEMBL + PubChem	Phase 4 (approved)	RARA, RARB, RARG
TRETINOIN	ChEMBL + PubChem	Phase 4 (approved)	RARA, RARB, RARG
TRIFAROTENE	ChEMBL + PubChem	Phase 4 (approved)	RARA, RARB, RARG
Zafirlukast	ChEMBL + PubChem	Phase 4 (approved)	RARA, RARB, RARG
TAMIBAROTENE	ChEMBL	Phase 4 (approved)	RARA, RARB, RARG
CONESSINE	ChEMBL	Phase 2	RARA, RARB, RARG
GLIQUIDONE	ChEMBL	Phase 2	RARA, RARB, RARG
Atorvastatin	PubChem	Approved	RARA, RARB, RARG
Bosentan	PubChem	Approved	RARA, RARB, RARG
Calcitriol	PubChem	Approved	RARA, RARB, RARG
Carprofen	PubChem	Approved	RARA, RARB, RARG
Diclofenac	PubChem	Approved	RARA, RARB, RARG
ethinyl estradiol	PubChem	Approved	RARA, RARB, RARG
Repaglinide	PubChem	Approved	RARA, RARB, RARG
rifampin	PubChem	Approved	RARA, RARB, RARG
Simvastatin	PubChem	Approved	RARA, RARB, RARG
Sunitinib	PubChem	Approved	RARA, RARB, RARG
Ticlopidine	PubChem	Approved	RARA, RARB, RARG
Verapamil	PubChem	Approved	RARA, RARB, RARG
TROGLITAZONE	ChEMBL	Phase 4 (approved)	RARB, RARG
Rivaroxaban	PubChem	Approved	RARB, RARG
IBUPROFEN	ChEMBL	Phase 4 (approved)	RARB
KETOCONAZOLE	ChEMBL	Phase 4 (approved)	RARB
RACECADOTRIL	ChEMBL	Phase 4 (approved)	RARG
TROVAFLOXACIN	ChEMBL	Phase 4 (approved)	RARB
MOLIBRESIB	ChEMBL	Phase 2	RARA
NRX195183	ChEMBL	Phase 2	RARA
arsenic trichloride	PubChem	Approved	RARA
arsenic triiodide	PubChem	Approved	RARA
Domperidone	PubChem	Approved	RARG
Pitavastatin	PubChem	Approved	RARG
Retinol	PubChem	Approved	RARA