padeliporfin

Action and Spectrum

Actions and Spectrum: 

padeliporfin is a photosensitizing agent in photodynamic therapy (PDT) to treat prostate cancer. PDT is a medical treatment that involves using a photosensitizing drug, like padeliporfin, combined with light to destroy cancer cells or abnormal tissues. 

• Photosensitization: padeliporfin is administered into the patient’s bloodstream, where it preferentially accumulates in cancerous or abnormal tissue due to the altered blood vessels and retention properties of these tissues. After a certain period, the drug concentration is higher in the targeted area compared to normal tissues. 
• Activation by Light: padeliporfin is activated by specific wavelengths of light. When light of the appropriate wavelength is applied to the treated area, padeliporfin absorbs the light energy. This absorption triggers reactions that generate reactive oxygen species (ROS), specifically singlet oxygen. ROS are highly reactive molecules that might damage cellular components, including membranes and proteins, leading to cell death. 
• Cellular Damage and Destruction: The singlet oxygen and other ROS generated due to the photoactivation of padeliporfin cause damage to the cancer cells’ structures and functions. This damage ultimately leads to cell death and the destruction of the targeted tissue. The goal is to selectively destroy the cancerous cells while sparing the surrounding healthy tissue to the extent possible. 

The action spectrum of padeliporfin refers to the range of wavelengths of light that are most effective in activating the drug and inducing the photodynamic reaction. The optimal wavelengths for padeliporfin activation can vary, but they are generally in the red light range (around 650 to 670 nanometers). This range of wavelengths allows padeliporfin to absorb light energy efficiently and generate the ROS necessary to destroy cancer cells. 

Drug Interaction

Adverse Reaction

Frequency not defined 

Pain and inability to pass urine 

frequent urination and incontinence 

Strong urge to pass urine 

Bleeding around the genital area 

Sexual problems like erectile dysfunction and ejaculation failure 

Urinary tract infection 

Blood in urine 

Black Box Warning

Black Box Warning: 

None 

Contraindication / Caution

Contraindication/Caution: 

Contraindication 

• Hypersensitivity: padeliporfin should not be used in individuals with known hypersensitivity or allergy to padeliporfin or its components. 
• Porphyria: padeliporfin should be avoided in patients with porphyria, a rare genetic disorder affecting the nervous system and skin. 
• Photosensitivity: Patients with known photosensitivity disorders may be at an enhanced risk of adverse reactions when exposed to light after receiving padeliporfin. The use of padeliporfin in such individuals should be carefully evaluated. 

Caution 

• Photosensitivity and Sun Protection: After receiving padeliporfin treatment, patients should be cautious about sun exposure for several days. The skin and eyes might be more sensitive to light, and direct exposure to sunlight or bright indoor light could cause discomfort or damage. Patients should follow the guidelines their healthcare provider provides for protecting their skin and eyes from light during this period. This may include wearing protective clothing and eyewear and using sunscreen. 
• Skin Reactions: Skin reactions are common after padeliporfin treatment and might include redness, swelling, pain, and peeling at the treatment site. Patients should be informed about these potential reactions and advised on managing them. It’s essential to report any severe or concerning reactions to the healthcare provider. 
• Eye Protection: Adequate eye protection should be worn as the healthcare provider recommends. This is to prevent eye damage from light exposure after padeliporfin treatment. 
• Medication and Medical History: Inform your healthcare provider about all medications, supplements, and medical conditions you have before undergoing padeliporfin treatment. Certain medications or medical conditions might interact with padeliporfin or increase the risk of adverse effects. 
• Underlying Medical Conditions: Individuals with the underlying medical conditions, such as liver or kidney problems, might require special consideration and monitoring during padeliporfin treatment. The healthcare provider should be aware of these conditions to ensure safe treatment. 
• Pregnancy and Breastfeeding: The safety of padeliporfin during pregnancy and breastfeeding has not been established. If you are pregnant, planning to become pregnant/breastfeeding, discuss the potential risks and also benefits with the healthcare provider before undergoing treatment. 
• Pediatric Use: padeliporfin in pediatric populations has not been well studied, and its safety and efficacy in children are not established. padeliporfin is primarily used in the treatment of prostate cancer in adult males. 
• Follow Healthcare Provider’s Instructions: It’s essential to closely follow the instructions which is provided by your healthcare provider regarding pre-treatment preparations, the treatment procedure, and post-treatment care.  

Pregnancy / Lactation

Pregnancy consideration:  

US FDA pregnancy category: Not assigned 

Lactation:   

Excreted into human milk: Not known. 

Pregnancy category: 

• Category A: well-controlled and Satisfactory studies show no risk to the fetus in the first or later trimester. 
• <b>Category B: there was no evidence of risk to the fetus in animal studies, and there were not enough studies on pregnant women. 
• Category C: there was evidence of risk of adverse effects in animal reproduction studies, and no adequate evidence in human studies must take care of potential risks in pregnant women.    
• Category D: adequate data with sufficient evidence of human fetal risk from various platforms, but despite the potential risk, and used only in emergency cases for potential benefits.    
• Category X: Drugs listed in this category outweigh the risks over benefits. Hence, these categories of drugs need to be avoided by pregnant women.    
• Category N: There is no data available for the drug under this category. 

Pharmacology

Pharmacology: 

padeliporfin is a photosensitizing photodynamic therapy (PDT) agent to treat localized prostate cancer. Administered intravenously, padeliporfin is selectively taken up by cancerous prostate tissue due to its affinity for tumor vasculature. Upon exposure to specific light wavelengths, padeliporfin undergoes photoactivation, producing reactive oxygen species that induce oxidative damage to targeted cancer cells.

This process ultimately results in cell death and the destruction of the malignant tissue while sparing surrounding healthy structures. The pharmacological action of padeliporfin centers on its selective accumulation and light-induced cytotoxic effects, making it a valuable tool in the localized treatment of prostate cancer. 

Pharmacodynamics: 

Mechanism of action: padeliporfin’s mechanism of action is rooted in its role as a photosensitizing agent used in photodynamic therapy (PDT). PDT is a treatment approach that involves the interaction between a photosensitizer (in this case, padeliporfin), light of a specific wavelength, and oxygen to destroy target cells, such as cancerous cells selectively.  

• Selective Accumulation: padeliporfin is administered intravenously and circulates throughout the bloodstream. It has an affinity for accumulating in specific tissues, often those with altered blood vessels seen in conditions like cancer. In the case of prostate cancer treatment, padeliporfin accumulates in the cancerous prostate tissue. 
• Photoactivation: After sufficient time has passed to allow padeliporfin to accumulate in the target tissue, a specific wavelength of light is applied to the treatment area. This light is usually delivered using external light sources or fiber-optic cables. 
• Reactive Oxygen Species (ROS) Generation: padeliporfin becomes excited upon exposure to the appropriate light wavelength and transitions to a higher energy state. This excited padeliporfin then interacts with molecular oxygen in the surrounding tissue to generate reactive oxygen species (ROS), primarily singlet oxygen.  
• Cellular Damage: The generated ROS, particularly singlet oxygen, cause damage to cellular structures within the target tissue. This damage includes lipid peroxidation of cell membranes, oxidation of proteins, and disruption of organelles. The cumulative effect is a breakdown of cellular integrity and function. 
• Cell Death and Tissue Destruction: The damage inflicted by ROS triggers a cascade of events that leads to cell death, both directly through cell membrane disruption and indirectly through cellular signaling pathways. In cancer treatment, the destruction of cancer cells is the desired outcome. 
• Immune Response and Tissue Clearance: The cellular damage and death caused by PDT initiate an immune response. Immune cells recognize the debris from dead cells and clear the damaged tissue. This immune response can contribute to the overall therapeutic effect of PDT. 

Pharmacokinetics: 

Absorption 

padeliporfin is administered as an intravenous (IV) infusion, which means it is directly introduced into the bloodstream. This allows for rapid drug distribution throughout the body, and it is generally well-absorbed into the blood following administration. 

Distribution 

After entering the bloodstream, padeliporfin is distributed to various tissues. The drug’s distribution might be influenced by blood flow, tissue permeability, and binding to blood proteins. 

Metabolism 

padeliporfin undergoes metabolic processes in the body, typically involving enzymes in the liver. However, detailed information about the specific metabolic pathways and metabolites generated from padeliporfin was limited in the available information. 

Elimination and Excretion 

The available information did not extensively discuss the excretion pathway of padeliporfin and its metabolites. Metabolites are likely eliminated from the body through the liver, kidneys, and bile routes. 

Adminstartion

Administration: 

padeliporfin is administered through a process called photodynamic therapy (PDT). PDT involves using a photosensitizing agent, like padeliporfin, in combination with light to treat certain medical conditions, such as prostate cancer.  

Preparation and Injection: 

padeliporfin is administered as an intravenous (IV) infusion. This means it is injected directly into your arm or hand vein. 

The healthcare provider will prepare the appropriate padeliporfin dose based on your medical condition, body weight, and treatment plan. 

Drug Absorption: 

padeliporfin is preferentially absorbed by abnormal or cancerous tissue due to its unique properties. After the injection, the drug circulates in your bloodstream and accumulates in the targeted tissue. 

Activation with Light: 

Activation of padeliporfin occurs when it is exposed to specific wavelengths of light. The light activates the drug, causing it to produce reactive oxygen species (ROS), primarily singlet oxygen. 

The light used for activation is typically delivered through a light source, which may be an external device or fiber-optic cables inserted directly into the treatment area. 

Light Delivery: 

The light source is carefully positioned to target the area with the accumulated padeliporfin. 

The light is delivered for a specific duration, during which the padeliporfin absorbs the light energy and triggers the production of ROS. These ROS cause damage to the targeted tissue. 

Cellular Damage and Treatment Outcome: 

The ROS generated by the padeliporfin activation causes cellular damage to the cancerous or abnormal tissue. 

Over time, the damaged cells undergo a process of destruction, leading to the shrinkage or eradication of the treated tissue. 

Post-Treatment Care: 

After the procedure, you may be monitored by healthcare professionals to ensure there are no immediate adverse reactions or complications. 

You will be advised to protect the skin and eyes from light exposure, as they may be sensitive to light for some time after treatment. 

Patient Information Leaflet

Patient information leaflet 

Generic Name: padeliporfin 

Why do we use padeliporfin? 

padeliporfin is primarily used in medicine for a specific type of treatment known as photodynamic therapy (PDT). PDT involves using a photosensitizing agent, such as padeliporfin, combined with light to treat certain medical conditions. The light activates the photosensitizer, generating reactive oxygen species that cause damage to targeted cells or tissues.  

Treatment of Localized Prostate Cancer: 

One of the primary uses of padeliporfin is in treating localized prostate cancer, specifically in patients who are not suitable candidates for surgical process or other conventional treatments. 

padeliporfin is injected into the bloodstream and accumulates preferentially in cancerous prostate tissue. When exposed to specific wavelengths of light, the padeliporfin is activated and generates reactive oxygen species that damage the cancer cells, destroying them. 

Other Indications: 

padeliporfin has been investigated for use in other medical conditions beyond prostate cancer. Research and clinical trials have explored its potential in treating conditions like benign prostatic hyperplasia and certain types of solid tumors.