Doxercalciferol

Doxercalciferol is a synthetic vitamin D 2 analog that requires metabolic activation to form the active 1α,25-(OH) 2 D 2 metabolite, which binds to the vitamin D receptor (VDR) to result in the selective activation of vitamin D responsive pathways. Vitamin D and doxercalciferol have been shown to reduce PTH levels by inhibiting PTH synthesis and secretion.

• Doxercalciferol capsules are indicated for the treatment of secondary hyperparathyroidism in adult patients with Stage 3 or Stage 4 chronic kidney disease (CKD) and adult patients with CKD on dialysis. Doxercalciferol Capsules is a synthetic vitamin D 2 analog: Doxercalciferol capsules are indicated for the treatment of secondary hyperparathyroidism in adult patients with Stage 3 or Stage 4 chronic kidney disease (CKD) and adult patients with CKD on dialysis.ICD-10: N18.9

• Doxercalciferol is contraindicated in patients with: Hypercalcemia [see Warnings and Precautions ( 5.1 )] Vitamin D toxicity [see Warnings and Precautions ( 5.1 )] Known hypersensitivity to doxercalciferol or any of the inactive ingredients of doxercalciferol capsules; serious hypersensitivity reactions including anaphylaxis and angioedema have been reported [see Warnings and Precautions ( 5.3 ), Adverse Reactions ( 6.2 )].contraindicated

Before initiating treatment, ensure serum calcium is not above the upper limit of normal. ( 2.1 ) Dosage for doxercalciferol capsules in patients with: Stage 3 or 4 CKD: Initiate dosing at 1 mcg orally once daily. Maximum dose is 3.5 mcg once daily. ( 2.2 ) CKD on dialysis: Initiate dosing at 10 mcg orally three times weekly at dialysis (no more frequently than every other day). Maximum dose is 20 mcg three times weekly for a total of 60 mcg weekly. ( 2.3 ) Target the maintenance dose of doxercalciferol to intact parathyroid hormone (PTH) levels within the desired therapeutic range and serum calcium within normal limits. ( 2 ) See Full Prescribing Information for dose titration, laboratory monitoring, and important administration instructions. ( 2 ) 2.1 Prior to Initiation of Doxercalciferol Capsules Ensure serum calcium is not above the upper limit of normal before initiating treatment with doxercalciferol capsules [see Warnings and Precautions ( 5.1 )]. 2.2 Dosage Recommendations for Doxercalciferol Capsules in Patients with Stage 3 or 4 CKD Initiate doxercalciferol capsules at a dose of 1 mcg orally once daily. Target the maintenance dose of doxercalciferol to intact parathyroid hormone (PTH) levels within the desired therapeutic range and serum calcium within normal limits. Monitor serum calcium, phosphorus, and intact PTH levels at least every two weeks for 3 months after initiation of therapy or dose adjustment, then monthly for 3 months, and every 3 months thereafter. Titrate the dose of doxercalciferol capsules based on intact PTH.

Hypercalcemia: Can occur during treatment with doxercalciferol and can lead to cardiac arrhythmias and seizures. Severe hypercalcemia may require emergency attention. Risk may be increased when used concomitantly with high dose calcium preparations, thiazide diuretics, or vitamin D compounds. Monitor serum calcium prior to initiation and during treatment and adjust dose accordingly. ( 2 , 5.1 ) Digitalis Toxicity: Hypercalcemia increases the risk of digitalis toxicity. In patients using digitalis compounds, monitor serum calcium and patients for signs and symptoms of digitalis toxicity. Increase frequency of monitoring when initiating or adjusting the dose of doxercalciferol. ( 5.2 ) Serious Hypersensitivity Reactions: Anaphylaxis, with symptoms of angioedema, hypotension, unresponsiveness, chest discomfort, shortness of breath, and cardiopulmonary arrest, has been reported in hemodialysis patients after administration of doxercalciferol. Monitor patients upon treatment initiation for hypersensitivity reactions. Should a reaction occur, discontinue and treat. ( 5.3 ) Adynamic Bone Disease: May develop and increase risk of fractures if intact PTH levels are suppressed to abnormally low levels. Monitor intact PTH levels to avoid oversuppression and adjust dose if needed. ( 5.4 ) 5.1 Hypercalcemia Hypercalcemia may occur during doxercalciferol treatment. Acute hypercalcemia may increase the risk of cardiac arrhythmias and seizures and may potentiate the effect of digitalis on the heart [see Warnings and Precautions ( 5.2 )] .

The following adverse reactions are discussed in greater detail in another section of the label: Hypercalcemia [see Warnings and Precautions ( 5.1 )] Serious Hypersensitivity Reactions [see Warnings and Precautions ( 5.3 )] Adynamic Bone Disease [see Warnings and Precautions ( 5.4 )] The most common adverse reactions in patients with Stage 3 or 4 CKD (incidence >5%) were infection, urinary tract infection, chest pain, angina pectoris, constipation, dyspepsia, anemia, leukopenia, dehydration, edema, depression, hypertonia, insomnia, asthenia, paresthesia, cough increased, dyspnea, pruritus, sinusitis, and rhinitis. ( 6.1 ) The most common adverse reactions in patients with CKD on dialysis (incidence >5%) were headache, malaise, edema, nausea/vomiting, dyspnea, dizziness, pruritus, and bradycardia. ( 6.1 ) To report SUSPECTED ADVERSE REACTIONS, contact Avet Pharmaceuticals Inc. at 1-866-901-DRUG (3784) or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch. 6.1 Clinical Trials Experience Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in practice. Adverse reactions in patients with stage 3 or 4 CKD Doxercalciferol capsules have been evaluated in two placebo-controlled, double-blind 24 week studies in patients with Stage 3 or 4 CKD. Patients were treated with doxercalciferol capsules (n=27) or placebo (n=28) [see Clinical Studies ( 14.1 )] .

8.1 Pregnancy Risk Summary The limited available data with doxercalciferol in pregnant women are insufficient to identify a drug-associated risk for major birth defects, miscarriage or adverse maternal or fetal outcomes. There are risks to the mother and fetus associated with chronic kidney disease in pregnancy [see Clinical Considerations] . In reproduction studies in rats and rabbits administered doxercalciferol during organogenesis at up to 20 mcg/kg/day and 0.1 mcg/kg/day, respectively (approximately 25 times (rats) and less than (rabbits) the maximum recommended human oral dose of 60 mcg/week based on mcg/m 2 body surface area), no adverse developmental effects were observed [see Data] . The estimated background risk of major birth defects and miscarriage for the indicated population is unknown. In the U.S. general population, the estimated background risk of major birth defects and miscarriage in clinically recognized pregnancies is 2% to 4% and 15% to 20%, respectively. Clinical Considerations Disease-associated maternal and/or embryo/fetal risk Chronic kidney disease in pregnancy increases the risk for maternal hypertension and preeclampsia, miscarriage, preterm delivery polyhydramnios, stillbirth, and low-birth-weight infants.

Metabolism

Absorption In healthy volunteers, peak blood levels of 1α,25-(OH) 2 D 2 , the major metabolite of doxercalciferol, are attained at 8 hours after a single intravenous dose of doxercalciferol and at 11 to 12 hours following capsule doses. Elimination The mean elimination half-life of 1α,25-(OH) 2 D 2 after an oral dose is approximately 32 to 37 hours with a range of up to 96 hours.

Overdosage of doxercalciferol may lead to hypercalcemia, hypercalciuria, and hyperphosphatemia [see Warnings and Precautions ( 5.1 )] . The treatment of acute overdosage should consist of supportive measures and discontinuation of doxercalciferol administration. Serum calcium levels should be measured until normal. Based on similarities between doxercalciferol and its active metabolite, 1α,25-(OH) 2 D 2 , it is expected that doxercalciferol is not removed from the blood by dialysis.

• Sep 26, 2019ANDAANDA210452Gland
• Feb 7, 2020ANDAANDA211670Meitheal
• Sep 15, 2020ANDAANDA205360Avet
• Jan 24, 2022ANDAANDA213717Eugia Pharma
• Jun 15, 2023ANDAANDA215810Alembic

Reference statistics from the openFDA drug-shortage dataset. For a live view, consult the FDA database directly. Not clinical guidance.

• Hectorol, Injection, 2 mcg/mL injection 50 single-dose vials (NDC 58468-0126-1)To be discontinued
  Sponsor: Sanofi-Aventis U.S. LLC
  Updated Dec 10, 2025
• Hectorol, Injection, 4 mcg/2 mL injection 50 multiple-dose vials (NDC 58468-0127-1)To be discontinued
  Sponsor: Sanofi-Aventis U.S. LLC
  Updated Dec 10, 2025
• Hectorol, Injection, 4 mcg/2 mL injection 50 single-dose vials (NDC 58468-0123-1)To be discontinued
  Sponsor: Sanofi-Aventis U.S. LLC
  Updated Dec 10, 2025

1. 1Dyspnoea137.9%
2. 2Acute Kidney Injury127.3%
3. 3Fatigue127.3%
4. 4Renal Failure127.3%
5. 5End Stage Renal Disease116.7%
6. 6Vomiting116.7%
7. 7Chronic Kidney Disease106.1%
8. 8Drug Hypersensitivity106.1%
9. 9Nausea95.5%
10. 10Anxiety84.8%
11. 11Asthenia84.8%
12. 12Pain84.8%
13. 13Unresponsive To Stimuli84.8%
14. 14Chest Pain74.2%
15. 15Diarrhoea74.2%

The 10 most recently updated of 26 ClinicalTrials.gov registrations naming Doxercalciferol as an intervention. Registration is not evidence of efficacy or safety — reference crosswalk only.

• Comparative Effects of Doxercalciferol and Calcitriol on Secondary Hyperparathyroidism in ESRD
  Not yet recruiting · Interventional · 98 enrolled · Chittagong Medical College
  NCT07640347updated 2026-06-10
• Safety and Efficacy of Hectorol in Pediatric Patients With Chronic Kidney Disease Stage 3 and 4 With Secondary Hyperparathyroidism Not Yet on Dialysis
  Terminated · Phase 3 · Interventional · 21 enrolled · Sanofi
  NCT02859896updated 2025-07-29
• Vitamin D and Carboxy PTH Fragments in Coronary Calcification
  Withdrawn · Phase 4 · Interventional · 0 enrolled · Southeast Renal Research Institute
  NCT00502268updated 2020-12-23
• Study of Docetaxel With Doxercalciferol or Placebo for Advanced Prostate Cancer
  Terminated · Phase 2 · Interventional · 70 enrolled · University of Wisconsin, Madison
  NCT00582582updated 2019-12-13
• Doxercalciferol Before Surgery in Treating Localized Prostate Cancer
  Completed · Phase 2 · Interventional · 60 enrolled · University of Wisconsin, Madison
  NCT00022412updated 2019-12-13
• Doxercalciferol in Treating Patients With Myelodysplastic Syndrome or Chronic Myelomonocytic Leukemia
  Completed · Phase 2 · Interventional · University of Wisconsin, Madison
  NCT00052832updated 2019-11-19
• Pilot Study Evaluating Doxercalciferol Replacement Therapy in Kidney Transplant Recipients
  Completed · Phase 4 · Interventional · 39 enrolled · Mariana Markell
  NCT00889629updated 2019-02-22
• Compare the Efficacy of Cinacalcet vs Traditional Vitamin D for Secondary Hyperparathyroidism (SHPT) Among Subjects Undergoing Hemodialysis
  Completed · Phase 4 · Interventional · 312 enrolled · Amgen
  NCT01181531updated 2018-10-17
• Trial to Optimize Mineral Outcomes in Dialysis Patients
  Completed · Phase 4 · Interventional · 92 enrolled · University of Colorado, Denver
  NCT01100723updated 2017-01-02
• Extension Study of CTAP101-CL-3001 or CTAP101-CL-3002
  Completed · Phase 3 · Interventional · 298 enrolled · OPKO Health, Inc.
  NCT02282813updated 2016-09-29

Frequently asked questions

How does Doxercalciferol work?

Doxercalciferol is a synthetic vitamin D 2 analog that requires metabolic activation to form the active 1α,25-(OH) 2 D 2 metabolite, which binds to the vitamin D receptor (VDR) to result in the selective activation of vitamin D responsive pathways. Vitamin D and doxercalciferol have been shown to reduce PTH levels by inhibiting PTH synthesis and secretion.

What is Doxercalciferol used for?

According to FDA labeling, Doxercalciferol carries indications including: Doxercalciferol capsules are indicated for the treatment of secondary hyperparathyroidism in adult patients with Stage 3 or Stage 4 chronic kidney disease (CKD) and adult patients with CKD on dialysis. Doxercalciferol Capsules is a synthetic vitamin D 2 analog: Doxercalciferol capsules are indicated for the treatment of secondary hyperparathyroidism in adult patients with Stage 3 or Stage 4 chronic kidney disease (CKD) and adult patients with CKD on dialysis.. This is a reference summary of labeled uses, not medical advice or a treatment recommendation.

What class of drug is Doxercalciferol?

Doxercalciferol is classified as Other anti-parathyroid agents, Vitamin D2 Analog, Enzyme Interactions, Bone Resorption Inhibition, Decreased PTH Secretion, Decreased Renal Ca++ Excretion, Stimulation Small Intestine Fluid/Electrolyte Absorption.

What are the brand names for Doxercalciferol?

Doxercalciferol is marketed under brand names including Hectorol.

What are the contraindications for Doxercalciferol?

Doxercalciferol labeling lists contraindications including: Doxercalciferol is contraindicated in patients with: Hypercalcemia [see Warnings and Precautions ( 5.1 )] Vitamin D toxicity [see Warnings and Precautions ( 5.1 )] Known hypersensitivity to doxercalciferol or any of the inactive ingredients of doxercalciferol capsules; serious hypersensitivity reactions including anaphylaxis and angioedema have been reported [see Warnings and Precautions ( 5.3 ), Adverse Reactions ( 6.2 )].. Always consult the full prescribing information and a clinician.