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Apoptone | CAS No: 183387-50-0 | GMP-certified suppliers
A medication that is investigated for cancer treatment, promoting tumor cell apoptosis and potentially overcoming multidrug resistance in various malignancies.
Therapeutic categories
Primary indications
- Investigated for use/treatment in cancer/tumors (unspecified)
Product Snapshot
- Apoptone is an investigational small molecule formulation intended for oncological applications
- Its primary therapeutic focus is the treatment of various cancer types or tumors
- Currently, Apoptone is in the investigational phase and does not hold approvals from major regulatory authorities such as FDA or EMA
Clinical Overview
Apoptone has been investigated for its potential clinical application in the treatment of tumors and various cancer types, though specific indications remain under exploration and it is currently considered an investigational agent. Its pharmacological profile is centered on antitumor activity achieved through modulation of apoptotic pathways.
Mechanistically, Apoptone acts as a second-generation antitumor agent that induces apoptosis in malignant cells. It functions primarily by inhibiting the BCL2 gene, which encodes proteins known to suppress programmed cell death, thereby facilitating apoptosis. Additionally, Apoptone downregulates the expression of ABCG2, also known as Breast Cancer Resistance Protein 1 (BCRP1), a transporter associated with multidrug resistance in cancer cells. This dual action not only promotes cancer cell death but may also contribute to overcoming chemoresistance.
Key ADME parameters for Apoptone have not been extensively described in available literature. As a steroid derivative, it is likely subject to hepatic metabolism and exhibits lipophilic characteristics, but specific absorption, distribution, metabolism, and excretion profiles require further elucidation.
Safety and toxicity data are limited due to its investigational status. Given its mechanism involving critical apoptotic regulators and transporter proteins, potential off-target effects and toxicities should be carefully evaluated in clinical studies. There are no approved branded formulations of Apoptone to date.
From an API sourcing perspective, due to its complex steroid structure, stringent quality control including stereochemical purity, impurity profiling, and compliance with established pharmacopeial standards is essential. Reliable manufacture under Good Manufacturing Practices (GMP) and secure supply chains are critical considerations for procurement in clinical and development contexts.
Identification & chemistry
| Generic name | Apoptone |
|---|---|
| Molecule type | Small molecule |
| CAS | 183387-50-0 |
| UNII | 891O182ZP5 |
| DrugBank ID | DB06307 |
Pharmacology
| Summary | HE3235 is a second-generation antitumor agent that induces apoptosis by inhibiting the BCL2 gene, reducing the expression of anti-apoptotic proteins while promoting pro-apoptotic factors. It also downregulates ABCG2, a gene encoding a protein associated with multi-drug resistance. These actions target tumor cell survival mechanisms and drug resistance pathways. |
|---|---|
| Mechanism of action | HE3235 is a second generation antitumor agent that causes apoptosis (cell death). HE3235 inhibits the BCL2 gene which translates proteins that prevent apoptosis and stimulates the expression proteins that induce apoptosis. HE3235 also downregulates the gene that codes for the multi-drug resistant protein ABCG2 (BCRP1 – Breast Cancer Resistance Protein1). |
Targets
| Target | Organism | Actions |
|---|---|---|
| Apoptosis regulator Bcl-2 | Humans |
Formulation & handling
- Apoptone is a small molecule androgen derivative with low aqueous solubility, suggesting formulation strategies should focus on enhancing bioavailability for oral administration. Its lipophilic nature (LogP 3.36) indicates potential challenges in achieving consistent dissolution rates. Stability considerations include protection from moisture due to its solid state and potential sensitivity during storage.
Regulatory status
Apoptone is a type of Hormones
Hormones are a vital category of pharmaceutical Active Pharmaceutical Ingredients (APIs) that play a crucial role in regulating various physiological processes in the human body. These chemical messengers are produced by endocrine glands and are responsible for maintaining homeostasis, growth, metabolism, and reproductive functions.
Pharmaceutical hormones are synthetic or naturally derived compounds that mimic the structure and function of endogenous hormones. They are widely used in the treatment of hormonal disorders, such as hypothyroidism, diabetes, and hormonal imbalances.
Common examples of hormone APIs include insulin, thyroid hormones (such as levothyroxine), glucocorticoids (such as prednisone), and sex hormones (such as estrogen and testosterone). These APIs are carefully synthesized, purified, and formulated to ensure optimal efficacy, stability, and bioavailability.
Hormone APIs are typically produced through advanced chemical synthesis or biotechnological processes, involving the use of genetically engineered microorganisms or mammalian cell cultures. Stringent quality control measures and regulatory guidelines ensure the purity, potency, and safety of hormone APIs.
Pharmaceutical companies and research institutions invest significant resources in developing hormone APIs, as they are fundamental for the treatment of various endocrine disorders. The demand for hormone APIs continues to grow, driven by the rising prevalence of hormonal diseases and an aging population.
In conclusion, hormone APIs are essential components of pharmaceuticals that help restore hormonal balance and alleviate various endocrine disorders. Their significance in healthcare makes them a crucial category in the pharmaceutical industry.
