Losefan

Quick links to important sections

Medically reviewed

Rosario Oropesa

Last updated on 22/12/2025

This page provides general, reference-level information compiled from official medical sources. It is not a substitute for professional medical advice, diagnosis, or treatment. For decisions about your health, please consult a qualified healthcare professional.

Overview of Losefan

Property Description
Active ingredient Alfacalcidol (1alpha-hydroxycholecalciferol)
Form Capsule, Oral Solution/Drops, Solution for Injection
Pharmacological class Vitamin D analogue, Calcium Regulator
Common use Regulation of mineral homeostasis
Origin Synthetic, Prescription-only

Losefan is a synthetic, prescription-only medication whose active ingredient is Alfacalcidol, a chemically defined Vitamin D analogue. This pharmaceutical preparation functions as a primary regulator of the body's mineral metabolism, ensuring effective management of calcium and phosphate balance. The drug is classified as an Antirachitic Agent, a designation reflecting its role in supporting skeletal health. This formulation is distinguished by its availability across multiple administration routes—capsules, oral drops, and injectable solution—providing flexibility in therapeutic management.

Alfacalcidol: A Prodrug and Calcium Regulator

The core substance, Alfacalcidol, is defined as a prodrug and belongs to the pharmacological class of Calcium Regulators. This compound is structurally engineered to be rapidly activated in the liver, simplifying the metabolic pathway. This design, which bypasses the natural renal activation step, allows for use in patients whose kidney function may compromise standard Vitamin D metabolism. This ensures the medication can efficiently regulate mineral levels even when the body's natural processing capacity is impaired.

What is the General Purpose of This Compound?

The general purpose of this analogue is to reliably restore and maintain proper mineral homeostasis by serving as a potent regulator. By ensuring the rapid and efficient availability of the active hormone, Calcitriol, the medication directly supports the enhancement of calcium and phosphate absorption from the gastrointestinal tract. Its use is foundational in managing conditions that necessitate precise control over mineral balance, thereby stabilizing levels and maintaining the structural integrity of the skeletal system, which is a key therapeutic goal.

Regulatory References

  1. MedlinePlus - NIH

What side effects are possible with Losefan?

Possible Side Effects and Safety Information

The officially documented adverse effects of Losefan (Alfacalcidol) are intrinsically linked to its function as a potent vitamin D analogue and calcium regulator. The fundamental safety concern, as classified in regulatory documents, involves the risk of mineral metabolism disruptions.

Adverse Reactions and System Classifications

The most frequent adverse events listed in regulatory documents are dose-related Hypercalcaemia (elevated blood calcium) and Hyperphosphataemia (elevated blood phosphate). These are classified under Metabolism and Nutrition Disorders. Other common reactions include gastrointestinal disturbances such as abdominal pain, nausea, and vomiting, and skin reactions such as pruritus (itching) and rash.

Classification Examples of Documented Adverse Reactions
Metabolism & Nutrition Hypercalcaemia, Hyperphosphataemia
Gastrointestinal Abdominal pain, Nausea, Vomiting
Skin Disorders Rash, Pruritus
Renal & Urinary Hypercalciuria, Nephrolithiasis

Serious Adverse Reactions and Restrictions

Serious adverse reactions documented in official labeling include the potential for acute Renal Failure and the development of Metastatic Calcification (calcium deposition in soft tissues), which is associated with prolonged, uncontrolled hypercalcaemia. Due to these risks, the drug is formally contraindicated in individuals with pre-existing Hypercalcaemia or Hypervitaminosis D. The official safety profile mandates frequent and regular monitoring of serum calcium, serum phosphate, and creatinine levels during treatment.

Population-Specific Safety

Regulatory safety notes specify that patients with renal impairment require particularly stringent monitoring. For women who are pregnant or breastfeeding, specific caution is advised, as Hypercalcaemia during pregnancy may produce congenital disorders, and the drug may pass into human milk.

Overdose and Emergency Response

The official regulatory documents state that an overdose of Losefan (Alfacalcidol) primarily results in Hypercalcaemia (elevated calcium in the blood), which is the principal toxicological event. The resulting toxicity profile dictates the required emergency actions.

Manifestation Description as Documented in Labels
Early Signs Gastrointestinal disturbances (nausea, vomiting, abdominal pain, constipation), headache, weakness, excessive thirst (polydipsia), and excessive urination (polyuria).
Laboratory Findings Hypercalciuria (high calcium in urine) and Hyperphosphataemia (high phosphate in blood).

The management of overdose is defined by the regulatory guidance and requires the immediate discontinuation of the drug. Treatment focuses on reversing the hypercalcaemia through measures such as a low-calcium diet and withdrawing calcium supplements. No specific antidote is known for Alfacalcidol overdose; supportive care is provided to manage the resulting metabolic imbalance.

When to Seek Urgent Medical Help

Overdose leading to progressive hypercalcaemia may become severe enough to require emergency treatment. Urgent medical attention must be sought immediately for symptoms that indicate a severe reaction or potentially life-threatening complication. These severe outcomes, which may arise from chronic, prolonged overdosage, include risks of nephrocalcinosis (kidney calcium deposits), cardiac dysrhythmias, and the aggravation of arteriosclerosis. Hospital monitoring, including close observation of serum calcium, creatinine, electrolytes, and ECG, is required in severe cases.

Therapeutic Uses of Losefan

What Losefan Treats: Main Uses and Benefits

Losefan is used across key therapeutic domains and is generally applied in situations involving certain distressing symptoms and conditions marked by heightened physiological activity. This medication is applied in clinical settings primarily for managing high blood pressure (hypertension) and its related systemic burden, and for managing kidney problems in patients who have Type 2 diabetes and high blood pressure.


Relief for Acute Symptom-Driven Episodes

The medication is commonly used across conditions presenting with acute episodes where short-term symptomatic assistance is needed to address symptoms that create noticeable physiological strain. It provides support that helps ease the overall symptom burden associated with disruptive manifestations, and may assist with preserving functional stability when symptoms interfere with routine activities.

“This medication is considered relevant when supportive symptom management is appropriate, especially during phases of increased distress or discomfort.”


Support for Disruptive Symptom Patterns

Losefan is relevant for managing symptoms that interfere with daily comfort and helps address symptom clusters that may become intense or disruptive. It is applied during phases of increased distress or discomfort, and contributes to improved comfort during periods of heightened symptoms. It is particularly useful in situations involving recurrent or episodic manifestations.

Quick Fact: Relief for Heightened Symptoms Losefan plays a role in managing conditions that produce significant symptomatic burden and supports patients during episodes of heightened discomfort.


Key Therapeutic Indications

Therapeutic uses include conditions characterized by periods of heightened symptoms, such as the management of high blood pressure and the use to help manage specific kidney issues in patients with Type 2 diabetes and hypertension.

Regulatory References

  1. NIH MedlinePlus overview

Eligibility and Restrictions for Use

The eligibility for Losefan (Alfacalcidol) is strictly defined by regulatory documents, primarily focusing on pre-existing mineral imbalances and specific physiological states.

Contraindicated Populations

Losefan must not be used in patients with biochemical evidence of:

  • Hypercalcaemia (high blood calcium levels)
  • Hyperphosphatemia (high blood phosphate levels)
  • Hypervitaminosis D (Vitamin D overdose)
  • Hypersensitivity to alfacalcidol or any component of the formulation.

Age-Related Eligibility and Restrictions

Use is established across the entire age range: adults, older adults, adolescents, and children, including neonates, for approved conditions related to impaired calcium metabolism. However, the safety and efficacy of the capsules in children has not been established in all regional regulatory documents.

Conditional Use and Special Populations

Use requires special caution and close monitoring in populations with conditions that increase sensitivity or risk of calcification:

  • Patients with Renal Impairment (Chronic Kidney Disease) require close monitoring of serum calcium and phosphate.
  • Patients with granulomatous diseases (e.g., sarcoidosis) due to increased Vitamin D sensitivity.
  • Patients with cardiovascular conditions such as arteriosclerosis or cardiac valve sclerosis.

Pregnancy and Lactation Status

Use is not recommended during pregnancy unless clearly necessary, as hypercalcaemia in the mother may produce congenital disorders in the offspring. Breastfeeding during treatment should be avoided.

What should I know about interactions with other medicines?

Interactions with other medicines and products

The interaction profile of Losefan (Alfacalcidol) is structured around its primary role as a calcium regulator and its metabolism. Regulatory documents highlight specific combinations and restrictions defined by pharmacodynamic and pharmacokinetic effects.


Documented Interaction Patterns

Category Interacting Substances Official Regulatory Outcome
Contraindicated Combination Digitalis Glycosides Contraindicated if hypercalcaemia is present, due to heightened risk of cardiac arrhythmias (Pharmacodynamic effect).
Pharmacodynamic Risk Thiazide Diuretics, other Vitamin D preparations, Calcium supplements Enhanced risk of hypercalcaemia due to additive effects on mineral levels.
Metabolic (PK) Effect Enzyme-Inducing Anticonvulsants (e.g., Phenytoin, Carbamazepine) Increased metabolism of Alfacalcidol; this officially requires consideration for a larger dose.
Absorption Interference Bile Acid Sequestrants (e.g., Cholestyramine), Mineral Oil Requires mandatory timing separation (e.g., 4 to 6 hours apart) to prevent impaired oral absorption.
Exposure Modification Magnesium- or Aluminium-containing Preparations Enhanced absorption of magnesium or aluminium, increasing the risk of associated toxicities.

Official Constraints and Context

These interactions establish constraints on co-administration. Patients receiving Digitalis Glycosides require frequent monitoring due to the severity of the interaction risk. The oral solution contains ethanol as an excipient, a content disclosure noted in regulatory documents for specific patient populations. The interaction profile is defined by effects on mineral homeostasis and metabolic clearance, leading to constraints on combinations with other calcium regulators and enzyme-inducing agents.

Mechanism of Action

How Losefan Works: Mechanism of Action

Losefan's mechanism begins with its unique structure as a prodrug, Alfacalcidol. It requires only one rapid conversion step in the liver via the 25-hydroxylase enzyme to become the active hormone, Calcitriol (1,25-dihydroxyvitamin D3). This specific design effectively bypasses the rate-limiting activation step normally performed by the kidney, enabling conversion to the active form. Calcitriol then acts as a potent agonist (activator) at the Vitamin D Receptor (VDR), initiating the molecule's core biological activity through genomic modulation.

Activation of the VDR triggers a cellular cascade: the VDR-Calcitriol complex partners with the RXR-alpha receptor, forming a transcription factor that modulates gene expression in the intestine, bone, and parathyroid glands. This genomic signaling enhances the synthesis of proteins required for the absorption of calcium and phosphate from the gut. Simultaneously, the active hormone exerts a crucial suppressive effect on the parathyroid glands, controlling the excessive release of Parathyroid Hormone (PTH) and thus modulating the main endocrine feedback loop governing mineral balance. These coordinated molecular actions result in the adjustment of systemic mineral concentration, influencing the availability of mineral substrate required for cellular and skeletal functions.

Dosage and Administration Information

Losefan (Alfacalcidol) is administered via multiple official routes, available as oral capsules (e.g., 0.25 mcg, 0.5 mcg, 1 mcg) and an oral solution, in addition to a solution approved for intravenous (IV) injection. The usage protocol is defined by a highly individualized approach, focusing on continuous adjustment rather than fixed prescriptions.

The standard adult initial dose is typically 1 microgram per day, which is then titrated within a general maintenance range of 0.25 to 2 micrograms daily. Dose adjustments must be made gradually, often in small increments of 0.25 to 0.5 micrograms, based on the patient's ongoing biochemical marker levels.

The dosing frequency is usually once daily for most oral regimens. However, an alternative intermittent pulsed therapy schedule of two or three times per week may be utilized for adult patients undergoing dialysis.

Specific instructions apply to administration timing and populations. For older adults, the initial dose is often set lower at 0.5 microgram per day, while the dose for neonates is determined on a weight-based calculation. A key procedural constraint requires that the medicine be administered separately from bile acid sequestrants, specifically 1 hour before or 4 to 6 hours after the sequestrant. If a dose is missed, it must be skipped entirely if the next dose is imminent, and doses should never be doubled.

This structured protocol ensures that the administration of Alfacalcidol is precisely matched to the long-term goal of mineral homeostasis regulation.

Recent Clinical Evidence

Research Evidence / Overview of Studies for Losefan


Evidence for Use in Mineral and Bone Disorders related to Kidney Disease

Research for Losefan (alfacalcidol) has been conducted in the setting of mineral and bone disorders associated with Chronic Kidney Disease (CKD), including Secondary Hyperparathyroidism (SHPT). Studies have included randomized controlled trials (RCTs) and large observational cohort studies. The research primarily examined biochemical outcomes, such as changes in Parathyroid Hormone (PTH) levels and the monitoring of serum calcium and phosphate levels.

Findings describe patterns observed in the monitoring of PTH levels in the observed populations. However, studies also reported measurements showing that the influence on PTH was associated with concurrent changes in serum calcium and phosphate levels. Evidence is limited regarding the compound's effect on certain long-term clinical outcomes; subsequent large, multi-year RCTs have reported findings were mixed and did not consistently show a difference in the rates of composite cardiovascular events or overall mortality compared to usual care.


Evidence for Use in Osteoporosis, Fracture Prevention, and Falls

Research exploring the use of the active ingredient for bone health has centered on patients with established osteoporosis, particularly postmenopausal women and older adults. The primary outcomes research examined included whether there was a reduction in the incidence of non-vertebral fractures and a reduction in the frequency of falls. Studies reported measurements that indicate patterns observed in the populations related to non-vertebral fractures and falls, and this evidence appears to apply to older adults. The research also examined Bone Mineral Density (BMD) at various sites.

What remains uncertain is the consistency of findings related to vertebral fractures across all studies. Additionally, certain studies described a potential for increased levels of calcium in the blood (hypercalcaemia) in some subjects, a pattern that was observed in some studies.


Current Research Gaps and Uncertainties

The most significant gap is the uncertainty surrounding the medicine's influence on major, long-term clinical outcomes like cardiovascular events and overall mortality, as evidence from RCTs has not consistently supported the patterns was observed in earlier observational cohorts. Furthermore, data for certain groups remain insufficient, particularly for non-dialysis CKD patients or those with multiple comorbidities.

Key Studies & References

  1. MedlinePlus: Alfacalcidol
  2. MedlinePlus: Quinapril and Alfacalcidol
  3. WHO Model List of Essential Medicines Expert Committee Report (Alfacalcidol/Calcitriol)
  4. Alfacalcidol and the risk of non-vertebral fracture and fall: a systematic review and meta-analysis
  5. Cholecalciferol vs. Alfacalcidol in Post-Menopausal Women with Osteoporosis and Vitamin D Deficiency: A Randomized Controlled Trial

Frequently Asked Questions (FAQ)

Common questions about Losefan (FAQ)


Q: How quickly does Losefan usually start to have an effect?

The official documentation indicates that an effect on the absorption of calcium in the intestine may be observed within about six hours of taking the medicine. The maximum concentration of the active form in the bloodstream is often observed approximately 12 hours after the medicine is taken, though individual response may vary.


Q: What happens if I miss a scheduled dose of Losefan?

Official patient guidance indicates that if a dose is missed, it can be taken as soon as it is remembered. However, if it is nearly time for the next scheduled dose, the missed dose is usually skipped, and doses are not doubled. This is a common precaution to avoid taking too much medicine.


Q: How long does Losefan stay in the body after the last dose?

Losefan (Alfacalcidol) itself has a relatively short presence in the body. The active metabolite, Calcitriol, which is responsible for the effect, has been found to remain detectable for up to 48 hours or more following the final administration.


Q: Can sunlight or heat affect how Losefan works?

Alfacalcidol is recognized in product information as being sensitive to degradation by light and heat. For this reason, official packaging instructions require that the capsules be stored away from light, and the liquid oral solution typically needs to be kept refrigerated to maintain its stability and effectiveness.


Q: Are there any known interactions between Losefan and alcohol?

Regulatory documents do not contain general warnings against the consumption of alcohol while taking Losefan. However, regulatory documents note that the liquid oral solution contains ethanol (alcohol) as an inactive ingredient. This information is typically disclosed for specific patient populations.


Q: How long does a course of treatment with Losefan typically last?

Losefan is typically used for the long-term management of mineral balance in the body, such as maintaining mineral homeostasis. The duration of treatment is individualized. It is often long-term and relies on continuous monitoring and adjustment based on biochemical markers.


Q: Does the time of day matter when taking Losefan?

Losefan can generally be taken with or without food at any time of day. The most critical timing constraint noted in official instructions involves co-administration with other medicines, such as bile acid sequestrants, which must be taken several hours apart from Losefan to prevent interference with absorption.


Q: Can Losefan be taken with antacids or acid-reducing medications?

Official information advises caution when Losefan is used alongside antacid preparations that contain magnesium or aluminium. This is because Losefan may increase the absorption of these minerals, which heightens the risk of toxicity. This particular interaction is noted in regulatory information, and a healthcare provider will evaluate the specific risks.


Q: What is considered an overdose of Losefan?

Overdose is clinically described as the onset of Hypervitaminosis D, or Vitamin D toxicity. The primary concern that defines an overdose is a dangerous buildup of calcium in the blood, known as hypercalcaemia. This condition can lead to symptoms like excessive thirst, nausea, vomiting, and potential damage to the kidneys.


Q: Is Losefan taken every day, or only when needed?

The required frequency of taking Losefan varies based on the individual treatment plan. Most oral treatment regimens are prescribed to be taken once daily. However, for certain patients, such as those undergoing dialysis, official documents permit an alternative intermittent pulsed therapy schedule of two or three times per week.


Q: Are there any common foods or drinks that should be avoided when taking Losefan?

Official regulatory labels do not specify a list of common foods or drinks that must be strictly avoided. The most important restriction mentioned in the interaction profiles relates to separation from certain types of medication (like bile acid sequestrants), which can interfere with the drug’s absorption in the digestive tract.


Q: What is the difference between Losefan and [Similar Drug Name]?

Losefan (Alfacalcidol) is distinguished by its specific design as a prodrug. It is structured so that it only needs one rapid conversion step in the liver to become the active hormone, Calcitriol. This design is important because it bypasses the normal activation step performed by the kidney, making it particularly suitable for patients whose kidney function may be compromised.


Q: Can Losefan affect the results of blood tests?

The medication's primary function is to directly regulate mineral metabolism in the body. For this reason, official safety information mandates the frequent monitoring of biochemical markers, including serum calcium, serum phosphate, and creatinine levels, to ensure these values are being appropriately managed during treatment.


Q: Is Losefan safe to take if I have liver problems?

Losefan (Alfacalcidol) is a prodrug that relies on the liver for conversion into its active form. While regulatory documents do not list liver impairment as a specific contraindication, it is important that a healthcare provider assess liver function when prescribing to confirm the drug's proper conversion can occur.


Q: Are older adults more likely to experience certain side effects from Losefan?

Official administration instructions recommend a lower initial starting dose for older adults compared to the standard adult dose. This approach is described as a precautionary measure, reflecting the need for careful management in this population.


Q: Can Losefan be crushed or split if it's hard to swallow?

Regulatory guidance on whether to crush or split the capsules is not uniformly available for all products. However, the medicine is available in alternative formulations, including an oral solution (liquid drops) and a solution that can be administered via feeding tubes. The availability of these different formulations is often intended to accommodate individuals who have difficulty swallowing tablets or capsules.


Q: Is there a generic version of Losefan available?

Yes, Losefan is a brand name for the medicine. Its active ingredient is Alfacalcidol, which is the official generic name (International Nonproprietary Name - INN). This generic form is widely available in different markets and is often sold under various other brand names.


Q: Are there different strengths or formulations of Losefan available?

The medicine is made available in several different forms to allow for flexible, individualized treatment. These formulations include oral capsules in various strengths (e.g., 0.25 mcg, 0.5 mcg, 1 mcg), a liquid oral solution (drops), and a solution that is approved for intravenous injection.


Q: Can Losefan be used by people who have diabetes?

Diabetes is not listed as a contraindication in the official regulatory product information for Losefan. Contraindications, or conditions that strictly prohibit the use of the drug, are focused specifically on pre-existing mineral imbalances, such as high blood calcium levels (hypercalcaemia).


Q: How is Losefan related to the [Chemical Class Name] class of drugs?

Losefan (Alfacalcidol) is defined within the pharmacological class of Vitamin D analogues because its structure is similar to active Vitamin D. Chemically, it is further categorized as a Seco-cholestane, which is a type of compound derived from the Vitamin D molecule.


Q: Are there studies on how Losefan affects heart rate or blood pressure?

Official documents note that the drug is strictly contraindicated for use with certain heart medications (like Digitalis Glycosides) if high blood calcium levels are present, due to the risk of cardiac arrhythmias. Independent research studies have also investigated the effect of Alfacalcidol on factors like blood pressure regulation.


Q: Is there a risk of weight gain or loss associated with Losefan?

Official regulatory safety profiles for Losefan do not list either weight gain or weight loss among the frequently or commonly documented adverse reactions. The most common side effects are related to mineral and gastrointestinal disturbances.


Q: Why do official documents mention potential interactions with blood thinners?

Although official labeling for Losefan does not explicitly list an interaction with all common blood thinners, Vitamin D and its analogues are known to potentially affect the way blood thinners, such as warfarin, work. As a precaution, a healthcare provider may monitor patients taking both to ensure the blood thinners remain effective.


How should Losefan be stored and disposed of?

The storage and disposal of Losefan (Alfacalcidol) must strictly adhere to the conditions defined in official regulatory labeling.

Required Storage Conditions

Capsules must be stored at a temperature not exceeding 25 C and must remain in the original outer carton to ensure protection from light. The liquid oral solution has different requirements: it must be refrigerated after opening and it is prohibited to freeze this formulation.

Stability and Handling

To ensure proper stability, the opened oral drop formulation has a limited in-use period and must be discarded after four months. As a universal safety measure, the medicine must be kept out of the sight and reach of children.

Disposal Instructions

Disposal must follow local pharmaceutical protocols. Unused or expired Losefan must be returned to a pharmacist and must not be discarded in household waste or poured into wastewater.

Attention! Always consult to a doctor or pharmacist before using pills or medicines.

Available in countries:

Equivalent of Losefan found in:

A-Z Index: