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Quinacrine | CAS No: 83-89-6 | GMP-certified suppliers
A medication that treats giardiasis, cutaneous leishmaniasis, and manages malignant effusions through antiparasitic and antimicrobial activities requiring precise API quality control for safe formulation.
Therapeutic categories
Primary indications
- For the treatment of giardiasis and cutaneous leishmaniasis and the management of malignant effusions
Product Snapshot
- Quinacrine is an oral small molecule formulation
- It is primarily indicated for the treatment of giardiasis, cutaneous leishmaniasis, and management of malignant effusions
- The compound currently holds investigational status and is not approved by major regulatory authorities
Clinical Overview
Pharmacodynamically, quinacrine exhibits antiparasitic and antibiotic properties. Its clinical efficacy in protozoal infections like giardiasis is established, though its precise mode of action is not fully elucidated. Quinacrine’s activity appears multifaceted, involving interference with parasite metabolism. Mechanistically, quinacrine intercalates into DNA by inserting between adjacent base pairs, disrupting transcription and RNA translation processes in vitro. However, it does not seem to accumulate in the nuclei of Giardia trophozoites, implying alternative membrane-associated or metabolic targets may contribute to its antimicrobial effects. The compound inhibits succinate oxidation and impairs electron transport, critical biochemical pathways in parasite survival. In autoimmune contexts such as lupus erythematosus, quinacrine binds nucleoproteins to suppress inflammatory cell factors and functions as a potent cholinesterase inhibitor.
Key ADME parameters are not fully characterized in current literature. Quinacrine is known to be a substrate for cytochrome P-450 enzymes, including CYP3A4 and CYP3A5 isoforms, with implications for metabolic interactions. It also acts as an inhibitor of P-glycoprotein and organic cation transporter 2 (OCT2), factors relevant to drug disposition and potential interactions.
Clinical use of quinacrine requires careful consideration of its safety profile. Toxicity concerns include possible dermatologic reactions, potential hematologic effects, and cholinergic disturbances due to enzyme inhibition. Its investigational status in many regions reflects limited recent approval and monitoring for adverse events.
For formulation scientists and sourcing professionals, stringent quality control of quinacrine API is essential, given its complex structure and potential for isomeric impurities. Reliable suppliers should provide comprehensive certificate of analysis documentation, including assays for purity, residual solvents, heavy metals, and adherence to pharmacopeial standards. Understanding CYP450 metabolism pathways and transporter inhibition is critical when integrating quinacrine into combination therapies or novel formulations.
Identification & chemistry
| Generic name | Quinacrine |
|---|---|
| Molecule type | Small molecule |
| CAS | 83-89-6 |
| UNII | H0C805XYDE |
| DrugBank ID | DB01103 |
Pharmacology
| Summary | Quinacrine exhibits antiparasitic activity primarily through interference with protozoal metabolism, including inhibition of succinate oxidation and disruption of electron transport. It binds to DNA via intercalation and interacts with nucleoproteins, affecting transcription and translation processes. Additionally, quinacrine inhibits certain phospholipase enzymes and cholinesterase, contributing to its therapeutic effects in giardiasis, cutaneous leishmaniasis, and malignant effusions. |
|---|---|
| Mechanism of action | The exact mechanism of antiparasitic action is unknown; however, quinacrine binds to deoxyribonucleic acid (DNA) in vitro by intercalation between adjacent base pairs, inhibiting transcription and translation to ribonucleic acid (RNA). Quinacrine does not appear to localize to the nucleus of Giaridia trophozoites, suggesting that DNA binding may not be the primary mechanism of its antimicrobial action. Fluorescence studies using Giardia suggest that the outer membranes may be involved. Quinacrine inhibits succinate oxidation and interferes with electron transport. In addition, by binding to nucleoproteins, quinacrine suppress the lupus erythematous cell factor and acts as a strong inhibitor of cholinesterase. |
| Pharmacodynamics | Quinacrine has been used as an antimalarial drug and as an antibiotic. It is used to treat giardiasis, a protozoal infection of the intestinal tract, and certain types of lupus erythematosus, an inflammatory disease that affects the joints, tendons, and other connective tissues and organs. Quinacrine may be injected into the space surrounding the lungs to prevent reoccurrence of pneumothorax. The exact way in which quinacrine works is unknown. It appears to interfere with the parasite's metabolism. |
Targets
| Target | Organism | Actions |
|---|---|---|
| DNA | Humans | intercalation |
| 85/88 kDa calcium-independent phospholipase A2 | Humans | inhibitor |
| Cytosolic phospholipase A2 | Humans | inhibitor |
ADME / PK
| Absorption | Absorbed rapidly from the gastrointestinal tract following oral administration. |
|---|---|
| Half-life | 5 to 14 days |
| Protein binding | 80-90% |
Formulation & handling
- Quinacrine is a small molecule with low aqueous solubility, indicating potential challenges in oral formulation absorption.
- Due to its high LogP, lipid-based formulations or solubilization strategies may be required to enhance bioavailability.
- As a solid acridine compound, standard solid-state stability precautions apply, with attention to avoiding light and moisture exposure during handling.
Regulatory status
Supply Chain
| Supply chain summary | Quinacrine is supplied primarily by originator companies with established manufacturing capabilities. Branded quinacrine products have a presence in the US and select international markets. Patent expirations indicate existing generic competition, facilitating broader sourcing opportunities within the API marketplace. |
|---|
Safety
| Toxicity | Oral, rat: LD<sub>50</sub> = 900 mg/kg; Oral, mouse: LD<sub>50</sub> = 1000 mg/kg. Symptoms of overdose include seizures, hypotension, cardiac arrhythmias, and cardiovascular collapse. |
|---|
- Toxicity classification based on oral LD50 values in rats (900 mg/kg) and mice (1000 mg/kg) indicates moderate acute toxicity
- Overdose exposure may result in central nervous system effects including seizures, along with cardiovascular disturbances such as hypotension, arrhythmias, and collapse
- Appropriate containment and handling procedures should be implemented to minimize exposure risk during manufacturing and processing
Quinacrine is a type of Antiprotozoics
Antiprotozoics are a vital subcategory of pharmaceutical Active Pharmaceutical Ingredients (APIs) used to combat protozoan infections. Protozoa are single-celled microorganisms that can cause severe diseases in humans, such as malaria, leishmaniasis, and toxoplasmosis. Antiprotozoic APIs play a crucial role in the development of effective medications to treat these infections.
These APIs work by targeting specific metabolic pathways or enzymes within the protozoan organisms, effectively inhibiting their growth and reproduction. By interrupting essential processes, antiprotozoics can eliminate the protozoa from the body or suppress their activity, allowing the immune system to effectively combat the infection.
Pharmaceutical companies invest significant efforts in research and development to discover and synthesize new antiprotozoic APIs. The goal is to develop highly potent and selective compounds that can effectively eradicate protozoa while minimizing side effects on the human body. This involves rigorous testing and screening of various chemical compounds to identify potential drug candidates with optimal therapeutic properties.
Antiprotozoic APIs are then used as the active ingredients in the formulation of pharmaceutical drugs, such as tablets, capsules, or injectables. These drugs are prescribed by healthcare professionals to patients suffering from protozoan infections. The selection of the appropriate antiprotozoic API depends on the specific protozoan strain and the characteristics of the infection.
In summary, antiprotozoic APIs are essential pharmaceutical ingredients that play a vital role in treating protozoan infections. Their development involves rigorous research and testing to identify potent compounds that can effectively target and eliminate protozoa, leading to improved health outcomes for patients.
Quinacrine (Antiprotozoics), classified under Antiparasitics
Antiparasitics are a category of pharmaceutical Active Pharmaceutical Ingredients (APIs) that are used to combat parasitic infections in humans and animals. These APIs play a crucial role in the field of medicine and veterinary care by targeting and eliminating various parasites, such as protozoa, helminths, and ectoparasites.
The use of antiparasitics is essential in preventing and treating parasitic diseases, which can cause significant health issues and even be life-threatening. These APIs work by interfering with the parasite's vital biological processes, such as reproduction, metabolism, and survival mechanisms.
Pharmaceutical companies develop and manufacture a wide range of antiparasitic APIs to cater to different parasitic infections. Some common examples of antiparasitics include anthelmintics (used against intestinal worms), antimalarials (used to treat malaria), and ectoparasiticides (used to control external parasites like ticks and fleas).
The development of antiparasitic APIs requires rigorous research, including the identification of suitable targets within the parasite's biology and the formulation of effective chemical compounds. Safety and efficacy are paramount in the manufacturing of antiparasitics, ensuring that they effectively combat the targeted parasites while minimizing adverse effects on the host.
Overall, antiparasitics are vital tools in the fight against parasitic infections, benefiting both human and animal health. Through ongoing research and development, the pharmaceutical industry continues to innovate and improve antiparasitic APIs, contributing to the advancement of healthcare and the well-being of individuals and their animal companions.
