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DRUG CLASS:

Tyrosinase inhibitor

3ms
Trial primary completion date
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BRAF (B-raf proto-oncogene)
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Libtayo (cemiplimab-rwlc) • BNT111
5ms
Expression of the tumor antigens NY-ESO-1, tyrosinase, MAGE-A3, and TPTE in pediatric and adult melanoma: a retrospective case control study. (PubMed, Virchows Arch)
BNT111, an investigational lipoplex-formulated mRNA-based therapeutic cancer vaccine encoding melanoma TAAs NY-ESO-1, tyrosinase, MAGE-A3, and TPTE, is undergoing clinical testing in adults. All four TAAs were expressed in pediatric melanoma, albeit NY-ESO-1 and MAGE-A3 to a lesser extent than in adult melanoma. These data support the possibility of investigating vaccines targeting these TAAs for the treatment of pediatric melanoma.
Retrospective data • Journal • IO biomarker
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CTAG1B (Cancer/testis antigen 1B)
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BNT111
1year
Enrollment closed
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BRAF (B-raf proto-oncogene)
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BRAF mutation • BRAF V600
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Libtayo (cemiplimab-rwlc) • BNT111
over1year
Trial With BNT111 and Cemiplimab in Combination or as Single Agents in Patients With Anti-PD-1-refractory/Relapsed, Unresectable Stage III or IV Melanoma (clinicaltrials.gov)
P2, N=180, Recruiting, BioNTech SE | Trial completion date: Jun 2025 --> Jul 2026 | Trial primary completion date: Oct 2024 --> Nov 2025
Trial completion date • Trial primary completion date
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BRAF (B-raf proto-oncogene)
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BRAF mutation • BRAF V600
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Libtayo (cemiplimab-rwlc) • BNT111
over1year
Trial completion • Metastases
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CTAG1B (Cancer/testis antigen 1B)
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BNT111
over1year
Discovery of amphotericin B, an antifungal drug as tyrosinase inhibitor with potent anti-melanogenic activity. (PubMed, Int J Biol Macromol)
Although hydroquinone, kojic acid, and arbutin are the most well-known tyrosinase inhibitors, their adverse effects are inevitable...Mechanistically, amphotericin B treatment significantly activated ERK and Akt signaling pathways, resulting in the decreased expression of MITF and tyrosinase. The obtained results may pursue pre-clinical and clinical studies to examine the possibility of using amphotericin B as an alternative treatment for hyperpigmentation disorders.
Journal
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MITF (Melanocyte Inducing Transcription Factor)
over1year
Homobimetallic Au(I)-Au(I) and Heterotrimetallic Au(I)-Fe(II)-Au(I) Complexes with Dialkyldithiophosphates and Phosphine Ligands: Structural Characterization, DFT Analysis, and Tyrosinase Inhibitory and Biological Effects. (PubMed, ACS Omega)
To investigate the possible cytotoxicities of 2, 3, and 7, in vitro cellular tests were carried out on the human cancerous breast cell line MCF-7. 2 and 7 show promising cytotoxicity.
Journal
over1year
Tripeptides conjugated with thiosemicarbazones: new inhibitors of tyrosinase for cosmeceutical use. (PubMed, J Enzyme Inhib Med Chem)
Mushroom tyrosinase was inhibited by TSC1-conjugates at micromolar level, with IC lower than this for kojic acid, a widely used reference compound. Up to now, this is the first report regarding thiosemicarbazones conjugated with tripeptides, synthesised for the purpose of tyrosinase inhibition.
Journal
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TSC1 (TSC complex subunit 1)
over1year
Ethyl Gallate Isolated from Castanopsis cuspidata var. sieboldii Branches Inhibits Melanogenesis and Promotes Autophagy in B16F10 Cells. (PubMed, Antioxidants (Basel))
In addition, EG downregulated melanogenetic gene expression and activated autophagy signals. Therefore, EG extracted from CCS branches could serve as a novel functional cosmetic material with antimelanogenic and autophagy-enhancing activity.
Journal
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MITF (Melanocyte Inducing Transcription Factor)
over1year
Upregulation of CD86 and IL-12 by rhododendrol in THP-1 cells cocultured with melanocytes through ROS and ATP. (PubMed, J Dermatol Sci)
RD is a pro-hapten sensitizer dependent on tyrosinase that induces ROS generation and ATP release from melanocytes for CD86 and IL-12 upregulation in DCs, possibly leading to the generation of tyrosinase-specific cytotoxic T lymphocytes. The coculture system h-CLATw/M may be useful for predicting the sensitizing potential to induce leukoderma.
Journal
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CD86 (CD86 Molecule)
almost2years
Evaluation and Comparison of the Antimelanogenic Properties of Different Solvent Fractionated Cnidium japonicum Extracts in B16F10 Murine Melanoma Cells. (PubMed, Prev Nutr Food Sci)
MeOH was the most active fraction to suppress the signaling pathway that produces tyrosinase. These results suggest that especially the MeOH fraction of C. japonicum extract serves as a potential source of bioactive substances, with effective antimelanogenesis properties.
Preclinical • Journal
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TYRP1 (Tyrosinase Related Protein 1) • MITF (Melanocyte Inducing Transcription Factor)
almost2years
Mechanism and inhibitory effects of cactus (Opuntia dillenii) extract on melanocytes and its potential application for whitening cosmetics. (PubMed, Sci Rep)
The cactus extract significantly inhibited tyrosinase activity and reduced melanin production, showing a whitening effect on skin tests. Cactus may be a good natural candidate for inhibiting melanin production and promoting cell proliferation.
Journal
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IGF1 (Insulin-like growth factor 1) • TGFB1 (Transforming Growth Factor Beta 1)
almost2years
Antimelanogenesis Effect of Methyl Gallate through the Regulation of PI3K/Akt and MEK/ERK in B16F10 Melanoma Cells. (PubMed, Evid Based Complement Alternat Med)
In conclusion, our findings indicated that activation of MEK/ERK and PI3K/Akt promoted by methyl gallate caused downregulation of MITF and triggered its downstream signaling pathway, thereby inhibiting the production of melanin. In summary, methyl gallate showed significant inhibitory activity against melanin formation, implying that it may be a potential ingredient for application in skin-whitening cosmetics.
Journal
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TYRP1 (Tyrosinase Related Protein 1) • DCT (Dopachrome Tautomerase) • MITF (Melanocyte Inducing Transcription Factor)
almost2years
Anti-Melanogenesis Effect of Polysaccharide from Saussurea involucrata on Forskolin-Induced Melanogenesis in B16F10 Melanoma Cells. (PubMed, Nutrients)
The anti-melanogenesis response of SIP might be attributed to the regulation of c-Jun N-terminal kinase (JNK) phosphorylation and β-catenin degradation pathways. These results suggest that polysaccharides from S. involucrata possess a strong anti-melanogenic effect, and thus could be used as a high-value natural material for skin whitening in cosmeceutical industries.
Journal
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TYRP1 (Tyrosinase Related Protein 1) • MITF (Melanocyte Inducing Transcription Factor) • MAPK8 (Mitogen-activated protein kinase 8)
2years
Investigating Potential Cardiovascular Toxicity of Two Anti-Leukemia Drugs of Asciminib and Ponatinib in Zebrafish Embryos. (PubMed, Int J Mol Sci)
We demonstrate that combining ASC with PON at no observed effect concentration (NOEC) did not cause any significant change in the cardiac performance parameter in zebrafish. However, a significant increase in nkx2.5 expression level and a substantial decrease in blood flow velocity were recorded, suggesting that combining these compounds at NOEC can cause mild cardiovascular-related side effects.
Journal
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ABL1 (ABL proto-oncogene 1) • BCR (BCR Activator Of RhoGEF And GTPase)
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BCR-ABL1 T315I • ABL1 T315I • BCR-ABL1 mutation
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Iclusig (ponatinib) • Scemblix (asciminib)
2years
The melanin inhibitory effect of plants and phytochemicals: A systematic review. (PubMed, Phytomedicine)
Although many plant extracts and phytochemicals have been found to inhibit melanin production, most of the results were only proved in cellular and/or animal models. Only the ethyl acetate extract of Oryza sativa Indica cv. panicle, and ginsenoside F1 were proved effective in human trials. Animal studies proved the effectiveness of galangin, origanoside, ginsenoside Rb1 and 4‑hydroxy-3-methoxycinnamaldehyde with effective dose below 3 mM, and therefore recommended for future human trial. In addition, cellular studies have demonstrated the effectiveness of oxyresveratrol, mulberroside A, kurarinol, kuraridinol, plumbagin, (6aR,11aR)-3,8-dihydroxy-9‑methoxy pterocarpan, ginsenoside Rh4, cardamonin, nobiletin, curcumin, β-mangostin and emodin in inhibiting melanin synthesis at low concentrations of 20 µM and proved the low SPF values of Dimorphandra gardneriana, Dimorphandra gardneriana, Lippia microphylla and Schinus terebinthifolius extracts, and therefore recommended for further animal and human trials.
Review • Journal
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MITF (Melanocyte Inducing Transcription Factor)
2years
A network pharmacology approach to evaluate the synergistic effect of dihydromyricetin and myricitrin in vine tea on the proliferation of B16F10 cells. (PubMed, Front Nutr)
We found that DMY and MYT induced apoptosis of B16F10 cells, and their combined application had a significant synergistic effect. The present findings indicated that vine tea had a multi-pathway and multi-target impact on the prevention and treatment of melanoma.
Journal
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TP53 (Tumor protein P53)
2years
Nomilin from Yuzu Seed Has In Vitro Antioxidant Activity and Downregulates Melanogenesis in B16F10 Melanoma Cells through the PKA/CREB Signaling Pathway. (PubMed, Antioxidants (Basel))
Nomilin significantly reduced the levels of p-CREB and p-PKA at the protein level and decreased the levels of skin-whitening-related factors MITF, tyrosinase, TRP-1, and TRP-2 at the mRNA level in a concentration-dependent manner. Thus, nomilin from yuzu seed husk can be used as a skin-whitening agent in cosmetics.
Preclinical • Journal
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MITF (Melanocyte Inducing Transcription Factor)
2years
Synthesis, biological evaluation, migratory inhibition and docking study of Indenopyrazolones as potential anticancer agents. (PubMed, Chem Biodivers)
Among all compounds, screened for anticancer activity, three compounds 4e, 4f and 4h reduced the cell proliferation significantly comparable to that of the positive standard drug erlotinib (IC =418.9±1.54 μM) with IC values ranging from 20.72-29.35 μM...The compounds 4b , 4f and 4h exhibited moderate tyrosinase inhibition effect as compared to α-MSH. Collectively, compound 4h can be considered as a candidate for further optimization in the development of anticancer therapies based on the results of biological investigations in this study.
Journal
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BRAF (B-raf proto-oncogene) • MMP2 (Matrix metallopeptidase 2) • PTGS2 (Prostaglandin-Endoperoxide Synthase 2)
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PTGS2 expression
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erlotinib
2years
Targeting co-delivery of doxorubicin and gefitinib by biotinylated Au NCs for overcoming multidrug resistance in imaging-guided anticancer therapy. (PubMed, Colloids Surf B Biointerfaces)
In addition, the dual-drug delivery system produced excellent synergistic therapeutic effects without extra adverse toxicities. It provides a reference for the design and clinical application of the dual-drug delivery system.
Journal
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EGFR (Epidermal growth factor receptor)
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EGFR mutation
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gefitinib • doxorubicin hydrochloride
over2years
Hirsutanone Isolated from the Bark of Alnus japonica Attenuates Melanogenesis via Dual Inhibition of Tyrosinase Activity and Expression of Melanogenic Proteins. (PubMed, Plants (Basel))
Hir also led to the suppression of cAMP response element-binding protein (CREB) phosphorylation and microphthalmia-associated transcription factor (MITF) expression, which control the expression of melanogenic enzymes. These results suggest that Hir suppressed melanin synthesis by dual inhibition of tyrosinase activity and the CREB/MITF pathway leading to the expression of melanogenic enzymes and may be a potent cosmetic and therapeutic agent for hyperpigmentation disorders.
Journal
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MITF (Melanocyte Inducing Transcription Factor)
over2years
Discovery of a Multifunctional Octapeptide from Lingzhi with Antioxidant and Tyrosinase Inhibitory Activity. (PubMed, Pharmaceuticals (Basel))
The Rab29 and Dct were upregulated whereas Tyrp1 was downregulated in the octapeptide treatment group. These findings could be used in the understanding of the molecular functions of the multifunctional octapeptide on melanogenic enzymes, supporting its potential as a therapeutic and cosmetic ingredient.
Journal
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TYRP1 (Tyrosinase Related Protein 1)
over2years
Identification of a Novel Class of Anti-Melanogenic Compounds, (Z)-5-(Substituted benzylidene)-3-phenyl-2-thioxothiazolidin-4-one Derivatives, and Their Reactive Oxygen Species Scavenging Activities. (PubMed, Antioxidants (Basel))
Furthermore, analog 2 not only reduced ROS levels, which induce melanogenesis, but it also suppressed tyrosinase and MITF (microphthalamia-associated transcription factor) protein levels and the expressions of melanogenesis-related genes. These results suggest that analog 2 is an efficient tyrosinase inhibitor that alleviates melanogenesis by dual mechanisms of (i) the inhibition of melanogenesis-related proteins and genes and (ii) the direct inhibition of tyrosinase activity.
Journal
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MITF (Melanocyte Inducing Transcription Factor)
over2years
Trial With BNT111 and Cemiplimab in Combination or as Single Agents in Patients With Anti-PD-1-refractory/Relapsed, Unresectable Stage III or IV Melanoma (clinicaltrials.gov)
P2, N=180, Recruiting, BioNTech SE | Trial completion date: Dec 2023 --> Jun 2025 | Trial primary completion date: May 2022 --> Oct 2024
Trial completion date • Trial primary completion date
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BRAF (B-raf proto-oncogene)
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BRAF mutation • BRAF V600
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Libtayo (cemiplimab-rwlc) • BNT111