Small-Molecule Drug Development Services for Cardiovascular Diseases

New therapeutic approaches for cardiovascular diseases have always been a hot topic in global pharmacy, and small-molecule drugs are one of the main directions. Ace Therapeutics has a comprehensive drug discovery platform to help clients conduct novel small-molecule drug discovery and development for cardiovascular diseases.

Traditional Small-Molecule Drugs for Cardiovascular Diseases

Small-molecule drugs play an important role in the treatment of cardiovascular disease. They are capable of targeting various aspects of cardiovascular physiology, including blood pressure regulation, cardiac rhythm stabilization, lipid metabolism, and thromboprophylaxis. Despite advances in biotechnology and biologics development, small-molecule drugs remain the main type of drug currently used in the clinical treatment of cardiovascular disease because of their efficacy, oral bioavailability, and typically low cost.

Table 1. Small-Molecule Drugs for Cardiovascular Diseases

In recent years, the research and development of innovative cardiovascular drugs has been the focus of attention in the pharmaceutical field. Ace Therapeutics provides clients with small-molecule drug discovery and development services for cardiovascular diseases from target identification to preclinical studies.

Target Identification and Validation

We can identify and validate potential targets for small-molecule drugs through genomic, transcriptomic, proteomic, and metabolomic databases of cardiovascular disease.

Hit Compound Identification

Typically, the identification of hit compounds is the beginning of small-molecule drug development. We can screen hit compounds for cardiovascular diseases through the following methods:

• Natural Products with Cardiovascular Protective Activity
  There are many plants or herbs whose constituents have been reported to have cardioprotective or cardiac regulatory activities. We can isolate and search for pharmacologically active monomer compounds from these plants and use them as potential hit compounds for new small-molecule drugs.
• Approved Drugs and Their Metabolites with Cardiovascular Pharmacological Effects
  Some approved drugs and their metabolites have been reported to exert pharmacological activity on the cardiovascular system. We may be able to identify potential lead compounds for cardiovascular drugs by exploring the avenues of drug repurposing derived from these approved drugs.
• Endogenous Cardiovascular Active Substances
  The role of endogenous cardiovascular actives in the regulation of the cardiovascular system is widely recognized. We can utilize these endogenous neurotransmitters, vasoactive peptides or enzyme substrates as potential hit compounds for cardiovascular drugs.
• Virtual Screening of Small-Molecule Compound Libraries
  We can utilize small-molecule compound libraries to find hit compounds using high throughput screening methods combined with computer-aided drug design.

Lead Compound Optimization

General cardiovascular drugs usually need to enter the body's blood circulation to exert their pharmacological effects. Therefore, we can optimize lead compounds to overcome the deficiencies present in the lead compounds and make them have significant pharmacological activity with ideal pharmacokinetic properties.

• Improvement for Solubility and Permeability
  For cardiovascular drugs administered by oral route, they need to be absorbed by the blood circulation to exert their drug efficacy. We can improve the solubility and bioavailability of lead compounds by introducing hydrophilic or lipophilic groups into the lead compounds to facilitate their absorption for oral administration.
• Improvement for Drug Targeting
  Cardiovascular drugs need to target specific receptor proteins, enzymes, or ion channels in the heart or blood vessels to exert their pharmacological effects. We can modify the lead compounds by pro-drug design or chemical structure modification to improve their targeting.
• Improvement for Drug Stability
  In clinical practice, the stability of cardiovascular drugs in the body's bloodstream is of vital importance for their efficacy. We can improve the physicochemical properties of lead compounds through pre-drug design to meet the stability requirements of cardiovascular drugs in vivo.

Preclinical Evaluation for Small-Molecule Drugs

We can perform pharmacodynamic, pharmacokinetic, and toxicity evaluations of small-molecule cardiovascular drugs in the early stages of drug development.

Ace Therapeutics is a contract research organization in the field of cardiovascular drug discovery and development. We are committed to providing customized small-molecule drug discovery and development services for cardiovascular diseases. If you are interested in our services, please don't hesitate to contact us.

1. Gyimesi, G.; Hediger, M.A. Transporter-Mediated Drug Delivery. Molecules. 2023, 28(3): 1151.