Doxercalciferol

HECTOROL

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Pronunciation: dox-er-kal-SIF-er-ol

Doxercalciferol ballicule: receptor binding, kinetics and half-life diagram — Mechanism of action: Doxercalciferol ballicule

What it isVitamin D2 prodrug requiring only hepatic activation; secondary hyperparathyroidism in CKD.

Why this oneIt bypasses the failing kidney while retaining some physiological regulation, unlike calcitriol.

What limits itHypercalcemia and hyperphosphatemia require monitoring. Oversuppression causes adynamic bone disease.

Doxercalciferol molecular structure (skeletal formula) — Molecular structure: Doxercalciferol

FDA-approved for

secondary hyperparathyroidism (1999)

FDA label

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FDA dosing	Population	Start	Target	Max
Secondary hyperparathyroidism, Stage 3–4 CKD	Adults	1 mcg QD	titrate to PTH	3.5 mcg QD
Secondary hyperparathyroidism, CKD on dialysis	Adults	10 mcg 3×/week at dialysis	titrate to PTH	20 mcg 3×/week (60 mcg/wk)

Titration Stage 3–4: may increase by 0.5 mcg at 2-week intervals based on intact PTH.

Renal Dose is defined by CKD stage / dialysis status (see dosing)

Hepatic May not metabolize normally; monitor intact PTH, calcium, phosphorus more frequently

Dialysis: three times weekly, no more frequently than every other day.

Instructions

Ensure serum calcium is not above the upper limit of normal before initiating.
Dialysis dosing: three times weekly, no more often than every other day.
Monitor calcium, phosphorus, and intact PTH; suspend or decrease dose if PTH abnormally low or calcium high; if suspended, restart after 1 week at ≥0.5 mcg lower.

Available strengths

cap 0.5, 1, 2.5 mcg
inj 2 mcg/mL

Contraindications

Hypercalcemia
Vitamin D toxicity

Cautions

Hypercalcemia (risk of arrhythmias, seizures); higher risk with calcium/thiazides/vitamin D compounds
Increased digitalis toxicity risk with hypercalcemia
Serious hypersensitivity/anaphylaxis reported in hemodialysis patients
Adynamic bone disease if PTH oversuppressed

Adverse reactions

Infection
UTI
Chest pain / angina
Constipation
Dyspepsia
Anemia
Edema
Dyspnea
Pruritus

Pregnancy Limited data insufficient to identify risk; CKD itself poses maternal/fetal risks

Lactation Undefined

Cost

Doxercalciferol (HECTOROL)

Strength		#/mo	CostPlus
0.5 mcg	cap	30 qd	offered
1 mcg	cap	30 qd	offered
2.5 mcg	cap	30 qd	offered
2 mcg/mL	inj	per unit	not offered

NADAC is a voluntary CMS survey of what retail community pharmacies pay for the drugs they stock. Doxercalciferol is administered under clinical supervision and dispensed outside retail pharmacies, so it rarely appears on surveyed invoices.

Generic entry2011

NO BOXED WARNINGS

Principal riskHypercalcemia; adynamic bone with oversuppression

Classes and tags

Clinical profile

Therapeutic safety burden2 / 4

Overdose danger1 / 4

Weight-gain liability0 / 4

Sedation liability0 / 4

QT / Torsades0 / 4

Direct muscarinic antagonism0 / 4

Embryofetal risk1 / 4

Legacy pregnancy categoryUnknown / historical label unavailable

Defining liabilityGenerally tolerated at therapeutic doses; clinically important risks are agent-specific and increase with interactions or organ impairment.

Active metabolites

Calcitriol

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