REMS restricted

Mycophenolate mofetil

CELLCEPT

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

Mycophenolate mofetil CELLCEPT mascot mnemonic cartoon — Visual mnemonic: Mycophenolate mofetil mascot
**“Michael found a late interCeption”**

What it isInhibitor of inosine monophosphate dehydrogenase, blocking lymphocyte purine synthesis; transplant and autoimmune disease.

Why this oneLymphocyte-selective, so it spares other marrow lines more than azathioprine, and it has replaced it in most transplant regimens.

What limits itPowerfully teratogenic with a REMS and mandatory contraception. GI intolerance and leukopenia; it is not the same dose as the sodium salt.

Mycophenolate mofetil molecular structure (skeletal formula) — Molecular structure: Mycophenolate mofetil

FDA-approved for

prophylaxis of organ transplant rejection (1995)

Off-label

lupus nephritis
autoimmune hepatitis
myasthenia gravis

FDA label

Read the full label on DailyMed ↗

BOXED WARNING Embryofetal toxicity (first-trimester pregnancy loss & congenital malformations); increased risk of lymphoma and other malignancies (esp. skin); increased susceptibility to serious/opportunistic infections including HBV/HCV reactivation.

FDA dosing	Population	Start	Target	Max
Kidney transplant rejection prophylaxis	adult	1 g BID (PO or IV over ≥2 h)
Heart transplant rejection prophylaxis	adult	1.5 g BID (PO or IV over ≥2 h)
Liver transplant rejection prophylaxis	adult	1.5 g BID PO or 1 g BID IV over ≥2 h
Kidney transplant rejection prophylaxis	peds ≥3 months	600 mg/m² BID		2 g/day
Heart transplant rejection prophylaxis	peds ≥3 months	600 mg/m² BID	900 mg/m² BID	3 g/day
Liver transplant rejection prophylaxis	peds ≥3 months	600 mg/m² BID	900 mg/m² BID	3 g/day

Renal Kidney transplant with severe chronic graft impairment (GFR <25 mL/min/1.73m²): avoid doses >1 g BID

Hepatic No dose adjustment for kidney transplant patients with severe hepatic parenchymal disease

Doses >1 g BID avoided when GFR <25

Instructions

Give on an empty stomach (may give with food in stable patients if necessary)
Do not crush tablets or open/crush capsules; avoid inhaling or skin/mucosal contact with powder
IV over no less than 2 h — never rapid or bolus injection
Give initial dose within 24 h of transplant; IV only until oral tolerated, up to 14 days
Interrupt or reduce dose for neutropenia (ANC <1.3 ×10³/mcL)

Available strengths

tab 500 mg
cap 250 mg
DR tab 180, 360 mg
susp 200 mg/mL
inj 500 mg

Contraindications

Polysorbate 80 (TWEEN) allergy — IV formulation

Cautions

Neutropenia and pure red cell aplasia — monitor CBC
GI bleeding, ulceration, perforation
Avoid in hypoxanthine-guanine phosphoribosyl-transferase deficiency (Lesch-Nyhan/Kelley-Seegmiller)
Acute inflammatory syndrome
Hypersensitivity (angioedema, anaphylaxis)
Avoid live attenuated vaccines
No blood donation during and 6 wk after; no semen donation during and 90 days after

Adverse reactions

Diarrhea
Leukopenia
Infection (incl. opportunistic)
Vomiting
Anemia
Hypertension
Peripheral edema
Nausea

Pregnancy Increased risk of first-trimester pregnancy loss (45–49%) and multiple congenital malformations; avoid if safer options available

Lactation No human milk data; present in rat milk — risk to breastfed infant cannot be excluded

Cost

Mycophenolate mofetil (CELLCEPT)

What pharmacies pay · NADAC 9/30/26

Strength		#/mo	generic $/mo	CostPlus
500 mg	tab	60 BID	$15.80	offered

Generic entry2012

⚠ BOXED WARNINGS

Embryo-fetal toxicity
Malignancies and serious infections

Classes and tags

Clinical profile

Therapeutic safety burden4 / 4

Overdose danger2 / 4

Weight-gain liability0 / 4

Sedation liability0 / 4

QT / Torsades0 / 4

Direct muscarinic antagonism0 / 4

Embryofetal risk4 / 4

Legacy pregnancy categoryD

Defining liabilityMajor teratogenicity, myelosuppression and serious infection risk.

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