Solving serotonin-dependent diseases: next-generation TPH1 inhibitors
Our technology
Novel class of TPH1 inhibitors
Binding to the Trp (substrate) and BH4 (co-factor) binding pockets of TPH1 simultaneously.
Potent inhibition of 5-HT production in vitro and in vivo.
TRYPTO THERAPEUTICS is developing a set of novel, proprietary small molecules at TRL level 4 to treat serotonin-related diseases.
We have developed and patented a novel class of TPH inhibitors (TPHi) with nanomolar potency in vitro.
Our TPHi differ in their scaffold, binding mode, and potency from TPHi that are currently on the market or under clinical investigation.
The lead TPHi compound achieved readiness to transition from academic research towards a targeted pharmaceutical development.
Comprehensive data package:
Potency & selectivity in vitro
ADME / TOX in vitro
PK in vivo
PD in vivo
Safety and toxicity in vivo
Completed development milestones:
Suitable ADME / Tox
Oral PK profile
Reproduced Proof of Concept in PAH
CMC process established
Proof of Concept for CMC scalability
Strong IP protection
Target indications and pipelines focus
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Oncology
Pathologically high serotonin levels contribute to tumor growth and metastasis in Colorectal Cancer, as well as severe gastrointestinal and cardiac symptoms in NET tumor patients (Carcinoid Syndrome).
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Pulmonary & cardiovascular disorders
Increased peripheral serotonin levels contribute to pulmonary vessel remodeling and aggravate the disease progression in PAH and PH-LHD subtypes of pulmonary hypertension.
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Explorative: inflammatory and fibrotic diseases
Besides its pro-inflammatory function in Asthma and IBD, serotonin is pathogenetically relevant for different kinds of fibrotic diseases in the lungs, liver, skin, and kidneys.
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Explorative: Obesity and metabolism
Peripheral serotonin regulates metabolism, but might also contribute to local inflammatory processes and fibrotic changes in the liver.
Our key publications
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TPT‐004, a Next‐Generation Inhibitor of Tryptophan Hydroxylase, Ameliorates Pulmonary Arterial Hypertension in Rats
Journal of the American Heart Association
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Novel Tryptophan Hydroxylase Inhibitor TPT-001 Reverses PAH, Vascular Remodeling, and Proliferative-Proinflammatory Gene Expression
JACC: Basic to Translational Science
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Structure-Based Design of Xanthine-Imidazopyridines and -Imidazothiazoles as Highly Potent and In Vivo Efficacious Tryptophan Hydroxylase Inhibitors
Journal of Medicinal Chemistry
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Structure-Based Design of Xanthine-Benzimidazole Derivatives as Novel and Potent Tryptophan Hydroxylase Inhibitors
Journal of Medicinal Chemistry
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Inhibition of serotonin synthesis: A novel therapeutic paradigm
Pharmacology & Therapeutics
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Peripheral Serotonin Synthesis as a New Drug Target
Trends in Pharmacological Sciences