Tunlametinib

Summary

Tunlametinib (CHEMBL5095241) is a phase-3 clinical-stage small molecule; indicated across 4 conditions including melanoma and non-small cell lung carcinoma; with CIViC clinical evidence for 1 variant-indication association (e.g. MIGA1::BRAF Fusion in langerhans-cell histiocytosis).

At a glance

• Status: Max clinical phase 3 (not approved)
• Modality: Small molecule
• Indications: 4 conditions
• Clinical trials: 16
• Precision-oncology evidence (CIViC): 1 variant–indication association
• Chemistry: 491.3 Da · C16H12F2IN3O3S

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL5095241
Name	Tunlametinib
Type	Small molecule
Max phase	3
FDA approved	no
PubChem CID	71621329
Molecular formula	C16H12F2IN3O3S
Molecular weight	491.3
InChIKey	UFZJUVFSSINETF-UHFFFAOYSA-N

SMILES: C1=CC(=C(C=C1I)F)NC2=C(C3=C(C=C2C(=O)NOCCO)SC=N3)F

IUPAC name: 4-fluoro-5-(2-fluoro-4-iodoanilino)-N-(2-hydroxyethoxy)-1,3-benzothiazole-6-carboxamide

Also known as: Hl 085, HL-085, HL085, Tunlametinib, TUNLAMETINIB

Patent coverage: 125 distinct patent families (260 SureChEMBL compound mentions), from 3 matched compound structure(s). One matched structure accounts for 250 (96%) 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

No target linkage available.

Bioactivity

No ChEMBL bioactivity rows at pChembl ≥ 5 (expected for biologics / antibodies).

Target pathways

No target-pathway data for this drug (no mapped target genes).

Indications & clinical

Indications

4 diseases in clinical trials (phase 1–3, investigational — not approved indications). Highest ChEMBL trial phase per disease; a non-cancer approved use is occasionally logged at phase 3 here.

Disease (in trials)	Phase	MONDO	EFO
melanoma	3	MONDO:0005105	EFO:0000756
non-small cell lung carcinoma	2	MONDO:0005233	EFO:0003060
colorectal carcinoma	2	MONDO:0024331	EFO:1001951
neoplasm	1	MONDO:0005070	EFO:0000616

Clinical trials

Total trials: 16.

Phase distribution

Phase	Trials
PHASE2	9
PHASE1	4
PHASE4	1
PHASE3	1
PHASE1/PHASE2	1

Top trials by phase / activity

NCT	Phase	Status	Title
NCT07445022	PHASE4	RECRUITING	RWS of Tunlametinib in NRAS-Mutant Advanced Melanoma
NCT06008106	PHASE3	RECRUITING	Comparing Tunlametinib Capsules and Combination Chemotherapy in Advanced NRAS-mutant Melanoma
NCT05331105	PHASE2	RECRUITING	HL-085 in Adults With Neurofibromatosis Type 1 (NF1) and Inoperable Plexiform Neurofibromas
NCT06970353	PHASE2	RECRUITING	Phase II Trial of Tunlametinib in NRAS-Mutant Advanced Thyroid Cancer
NCT07170293	PHASE2	RECRUITING	Phase II Trial of Tunlametinib in Patients With NRAS Mutant Non-melanoma Refractory Solid Tumors
NCT07463677	PHASE2	NOT_YET_RECRUITING	Tunlametinib Combination Therapy in KRAS-Mutated Unresectable Locally Advanced or Metastatic Non-Small Cell Lung Cancer
NCT07507526	PHASE2	NOT_YET_RECRUITING	A Study of Disitamab Vedotin, Tunlametinib, and PD-1 Antibody for Advanced Gastric Cancer
NCT03973151	PHASE1/PHASE2	COMPLETED	Study of HL-085 in NRAS Mutant Advanced Melanoma
NCT05217303	PHASE2	COMPLETED	HL-085 in NRAS-mutated Advanced Melanoma
NCT05233332	PHASE2	UNKNOWN	Study of HL-085 and Vemurafinib in Metastatic Colorectal Cancer (mCRC)
NCT05263453	PHASE2	UNKNOWN	HL-085+Vemurafenib to Treat Advanced Melanoma Patients With BRAF V600E/K Mutation
NCT05900219	PHASE2	UNKNOWN	Efficacy and Safety of HL-085 Combined With Vemurafenib in BRAF V600E Patients With Non-small Cell Lung Cancer: a Phase II Clinical Study
NCT03781219	PHASE1	UNKNOWN	A PhaseI Study of HL-085 Plus Vemurafenib in Solid Tumor With BRAF V600 Mutation
NCT03976050	PHASE1	TERMINATED	Phase I Study of HL-085 in Patients With Advanced Solid Tumors
NCT03990077	PHASE1	TERMINATED	Study of HL-085 Plus Docetaxel in Patients With KRAS Mutant NSCLC
NCT04683354	PHASE1	COMPLETED	Study of HL-085 in Patients With Advanced Solid Tumor Tumors

Clinical evidence (CIViC)

Variant × indication × effect (1 predictive associations from 1 curated evidence items):

Variant	Indication	Effect	Therapy	Level	CIViC
MIGA1::BRAF Fusion	Langerhans-cell Histiocytosis	Sensitivity/Response	Tunlametinib + BRAF Inhibitor	CIViC D	EID8030

Pharmacology

Pharmacogenomics

No PharmGKB pharmacogenomic data curated for this drug.

Related molecules

Related molecules

No competitor molecules sharing a primary target (ChEMBL phase ≥2 or PubChem drug-class).