Rapacan
✅ Immunosuppressive Drug
✅ Prevents Organ Rejection
✅ Treats Lymphangioleiomyomatosis
✅ Reduces Kidney Damage
✅ Controls Rare Lung Disease
✓ Medisch beoordeeld door Morgan Ellis — Apotheekonderzoeker · 8 jaar ervaring · Laatst beoordeeld: mei 2026
⚡ Quick Answer — What is Rapacan?
Rapacan is an oral tablet from Biocon containing sirolimus 1 mg — an mTOR (mammalian target of rapamycin) inhibitor originally isolated from Streptomyces hygroscopicus on Easter Island (rapa nui — hence rapamycin). First-line maintenance immunosuppression in kidney transplant (with low-dose calcineurin inhibitor or as calcineurin-free regimen). Also FDA-approved for lymphangioleiomyomatosis (LAM), and used off-label in tuberous sclerosis complex (TSC)-related conditions including subependymal giant-cell astrocytoma (SEGA), renal angiomyolipoma, and skin manifestations. Standard transplant maintenance: 2–5 mg once daily with therapeutic drug monitoring (target trough 4–12 ng/mL depending on regimen). FDA black-box: increased mortality and hepatic artery thrombosis with liver transplant; bronchial anastomotic dehiscence with lung transplant. Mandatory: lipid panel, FBC, renal function, fasting glucose monitoring; pneumonitis surveillance. Lifetime sun protection (skin cancer signal).
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What Is Rapacan?
Rapacan is an oral tablet from Biocon containing sirolimus 1 mg. Sirolimus (also known as rapamycin) is a macrolide compound that binds the intracellular protein FKBP12 to form a complex that inhibits the mTOR (mammalian target of rapamycin) serine-threonine kinase. mTOR is a master regulator of cell growth, proliferation, and survival downstream of growth-factor and nutrient signalling. Sirolimus was originally developed by Wyeth and approved by the FDA in 1999 (brand name Rapamune). It is the parent compound of the structurally similar everolimus and temsirolimus.
How Does Rapacan Work?
- Sirolimus binds FKBP12 — the same intracellular receptor as tacrolimus (FK506). However, the sirolimus-FKBP12 complex inhibits a different downstream target (mTOR) versus tacrolimus-FKBP12 which inhibits calcineurin.
- mTOR inhibition blocks the IL-2-driven progression from G1 to S phase of the lymphocyte cell cycle — suppressing T-cell and B-cell proliferation without depleting them.
- Antifibrotic and antiangiogenic effects — mTOR inhibition reduces VEGF signalling and explains efficacy in LAM and TSC-related lesions.
- Distinct mechanism from calcineurin inhibitors — allows calcineurin-inhibitor minimisation or elimination in some transplant protocols, reducing nephrotoxicity in late-stage transplant maintenance.
Toepassingen en Indicaties
- Kidney transplant maintenance — from 2–4 months post-transplant onwards, with calcineurin-inhibitor minimisation or in calcineurin-free regimens. Particularly useful in patients with calcineurin-inhibitor nephrotoxicity.
- Lymphangioleiomyomatosis (LAM) — FDA-approved 2015 (MILES trial) — stabilises lung function in this rare progressive cystic lung disease almost exclusively affecting women.
- Tuberous sclerosis complex (TSC)-related lesions (off-label in some jurisdictions; everolimus is the on-label agent): subependymal giant-cell astrocytoma (SEGA), renal angiomyolipoma, facial angiofibromas (topical), refractory epilepsy.
- Pulmonary arterial hypertension (off-label): some specialist use.
- Drug-eluting coronary stents: sirolimus and analogues coat balloon-expandable stents to prevent restenosis (separate medical-device indication).
Rapacan is niet indicated for primary cancer treatment. The closely related everolimus has multiple oncology indications (HR+ HER2- breast cancer with exemestane, advanced renal cell carcinoma, neuroendocrine tumours, SEGA, TSC angiomyolipoma) but sirolimus itself is primarily transplant-focused.
Rapacan Dosage and How to Take
Standard maintenance dose: 2–5 mg once daily after a loading dose. Therapeutic drug monitoring is mandatory — target whole-blood trough concentration depends on indication and combination regimen.
| Indicatie | Dosing approach | Target trough (ng/mL) |
|---|---|---|
| Renal transplant + ciclosporin | 6 mg loading then 2 mg/day | 4–12 |
| Renal transplant calcineurin-free | 15 mg loading then 5 mg/day | 12–20 first year |
| LAM | 2 mg/day, titrate by trough | 5–15 |
| TSC angiomyolipoma / SEGA | Specialist titration | 5–15 (everolimus preferred) |
How to Take Rapacan Properly
- Once daily at the same time each day. Consistency is more important than morning vs evening.
- Take consistently with or without food. A high-fat meal increases AUC by ~35% and Cmax by ~65% — pick one and stick with it; do not switch between fed and fasted dosing as it changes trough levels.
- Swallow tablets whole with water. Do not crush, chew, or split.
- Mandatory monitoring: whole-blood trough sirolimus level (drawn 24 h after dose, immediately before next dose). Initial level at week 1, weekly until stable, then every 3–6 months. Lipid panel at baseline + monthly initially. FBC, LFTs, renal function, fasting glucose monthly initially.
- Skin protection: SPF 50+ sunscreen daily, broad-brimmed hat, long sleeves. Annual full-body dermatological examination — long-term mTOR inhibition increases skin cancer risk.
- Vaccinations: live vaccines (MMR, varicella, yellow fever, BCG) are gecontra-indiceerd. Inactivated vaccines (annual flu, COVID, pneumococcal) recommended.
- Wound care: sirolimus impairs wound healing. Stop temporarily before elective surgery (typically 2–4 weeks pre-op) and resume after wound is well-healed.
- Do not stop without specialist instruction.
Side Effects of Rapacan
Common (often dose-related):
- Hyperlipidaemia (cholesterol and triglyceride rises) — the dominant metabolic side effect; treat with statins
- Aphthous (oral) ulcers / mucositis — particularly early in treatment
- Acne and skin rash
- Perifeer oedeem
- Hypertensie
- Anaemia, thrombocytopenia, leucopenia
- Diarrhoea, nausea
- Hoofdpijn
- Joint pain
Important — trigger investigation or treatment hold:
- Pneumonitis (interstitial lung disease) — class effect of mTOR inhibitors. New-onset cough, dyspnoea, hypoxia: stop, chest CT, bronchoscopy, specialist review
- Severe wound-healing complications — dehiscence, lymphocele, infection. Hold around surgery
- Serious infections — CMV, BK virus, Pneumocystis, opportunistic fungal
- Proteinuria (especially in calcineurin-free regimens) — mandates dose adjustment or specialist review
- New-onset diabetes after transplant — the metabolic profile of sirolimus contributes
- Lymphoma and skin cancer — long-term immunosuppression risk; annual skin examination
Zeldzaam maar ernstig: hepatic artery thrombosis (FDA black-box; sirolimus avoided in liver transplant), bronchial anastomotic dehiscence (FDA black-box; sirolimus avoided in lung transplant), thrombotic microangiopathy.
Waarschuwingen en voorzorgsmaatregelen
- Liver transplantation: FDA black-box — increased mortality and hepatic artery thrombosis. Avoid in liver transplant.
- Lung transplantation: FDA black-box — bronchial anastomotic dehiscence. Avoid in lung transplant in the early post-operative period.
- Zwangerschap: contraindicated — teratogenic in animal models. Effective contraception throughout treatment + 12 weeks after stopping. Affects both male and female fertility.
- Borstvoeding: contraindicated.
- Live vaccines: contraindicated.
- Wound healing: stop 2–4 weeks before elective surgery; resume after wound is well-healed.
- Active serious infection: hold treatment.
- Ernstige leverfunctiestoornis: dose reduction by approximately one third; specialist supervision.
- Hyperlipidaemia: baseline + monthly lipid panel. Treat with statin if persistent — pravastatin or fluvastatin preferred (lowest CYP3A4 interaction).
- Skin cancer surveillance: annual full-body dermatology examination. Strict SPF 50+ daily.
- Heart transplant: mTOR inhibitor-pneumonitis risk — baseline pulmonary function tests + chest imaging if symptoms.
Geneesmiddelinteracties
Sirolimus is a CYP3A4 and P-gp substrate — many clinically important interactions.
| Combineren met | Effect | Wat te doen |
|---|---|---|
| Strong CYP3A4 inhibitors (ketoconazole, itraconazole, voriconazole, ritonavir, clarithromycin, grapefruit juice) | Sirolimus levels rise dramatically — toxicity | Avoid combination. If unavoidable, reduce sirolimus dose by 50–75% with intensive trough monitoring. |
| Strong CYP3A4 inducers (rifampicin, carbamazepine, phenytoin, phenobarbital, St John's wort) | Sirolimus levels collapse — rejection risk | Avoid combination. If unavoidable, increase sirolimus dose with intensive monitoring. |
| Ciclosporine | Ciclosporin raises sirolimus AUC — standard combination but timing-dependent | Take sirolimus 4 hours after ciclosporin. Standard transplant regimen with calcineurin-inhibitor minimisation. |
| Tacrolimus | Combined nephrotoxicity | Specialist combination only with intensive monitoring. |
| ACE-remmers | Risk of angioedema (additive with mTOR inhibition) | Caution — switch to ARB if angioedema occurs. |
| Statins (simvastatin, lovastatin) | Raised statin levels — myopathy risk | Switch to pravastatin, fluvastatin, or rosuvastatin (lower CYP3A4 dependence). |
| Live vaccines | Disseminated vaccine-strain infection risk | Contraindicated. |
| Grapefruitsap | CYP3A4 inhibition — sirolimus levels rise unpredictably | Avoid throughout treatment. |
Bewaaradvies
- Store at 2–8°C (refrigerated). Some formulations are stable at room temperature for limited periods — check pack label.
- Protect from light. Keep in original blister.
- Buiten bereik van kinderen en huisdieren houden.
- Return unused tablets to a pharmacy for disposal.
Waarom bestellen bij MedsBase
Elke batch wordt ingekocht bij een WHO-GMP gecertificeerde fabrikant. Bestellingen worden verzonden in eenvoudige, ongemarkeerde verpakkingen door onze logistieke partners en vallen onder onze Reshipment Assurance Policy: als een pakket niet binnen 20 werkdagen arriveert, sturen wij kosteloos een nieuwe zending, zonder vragen te stellen.
Related Medications
Other medications stocked alongside this product:
- Siromus (sirolimus 1 mg)
- Cellcept (mycophenolate mofetil 500 mg)
- Imutrex (methotrexate 2.5/7.5/10 mg)
- Folitrax (methotrexate 2.5/7.5/10 mg)
- Endoxan (cyclophosphamide 50 mg)
Veelgestelde vragen
Why is Rapacan listed under Anti-Cancer?
Sirolimus is primarily a transplant immunosuppressant. The mTOR pathway is implicated in multiple cancers and the structurally related everolimus has FDA approval for several oncology indications, but sirolimus itself is not a standard cancer drug. The current category placement appears to be a historical taxonomy issue.
Rapacan versus tacrolimus — which is better?
They have different mechanisms (mTOR vs calcineurin), different side-effect profiles, and different roles. Tacrolimus is the standard backbone for early post-transplant induction and maintenance. Sirolimus is typically introduced from 2–4 months post-transplant, often replacing or reducing tacrolimus, particularly in patients with calcineurin-inhibitor nephrotoxicity. They are not interchangeable.
Rapacan versus everolimus?
Everolimus is a sirolimus analogue with a hydroxyethyl modification that gives a shorter half-life (28 vs 60 hours) allowing twice-daily dosing and faster dose adjustment. Everolimus has more on-label indications (HR+ HER2- breast cancer with exemestane, advanced renal cell carcinoma, neuroendocrine tumours, SEGA, TSC-AML, drug-eluting stents). Sirolimus is the parent compound and remains widely used in transplant maintenance and LAM.
Will Rapacan increase my cancer risk?
Long-term immunosuppression with any agent (sirolimus, tacrolimus, ciclosporin, mycophenolate) increases lifetime risk of skin cancer, post-transplant lymphoproliferative disorder, and several other malignancies. The mTOR inhibitor class may have a een lager skin cancer risk than calcineurin inhibitors based on transplant cohort data — some centres switch patients with multiple skin cancers to sirolimus. Annual full-body skin examination + SPF 50+ daily is standard regardless of regimen.
Why do I need a sirolimus blood test?
Sirolimus has a narrow therapeutic window. Below the target trough you risk transplant rejection; above the target you risk pneumonitis, severe hyperlipidaemia, infection, and other toxicity. The 24-hour pre-dose trough on whole blood is the standard monitoring sample. Targets vary by indication and regimen — your transplant team will set yours.
Can I have an operation while on Rapacan?
Sirolimus impairs wound healing through mTOR inhibition of fibroblast and endothelial proliferation. For elective surgery, sirolimus is typically held for 2–4 weeks pre-op and resumed after the wound is well-healed (typically 2–4 weeks post-op). For emergency surgery, sirolimus is held immediately and a calcineurin-inhibitor-based regimen substituted under transplant team guidance.
Why do I need to take Rapacan consistently with or without food?
A high-fat meal increases sirolimus AUC by ~35% and peak by ~65%. If you switch between fed and fasted dosing, your trough levels become unpredictable. Pick a routine (most people prefer consistently fasting because it’s easier to be reproducible) and stick with it.
Are Rapacan and Siromus the same as Rapamune?
Yes — Rapacan, Siromus, and Rapamune are all sirolimus 1 mg. Rapamune is the original Wyeth/Pfizer brand. Rapacan and Siromus are bioequivalent generic versions from different manufacturers.
What is LAM?
Lymphangioleiomyomatosis is a rare progressive cystic lung disease that almost exclusively affects women, often associated with tuberous sclerosis. mTOR inhibition with sirolimus stabilises lung function (FEV1) in LAM — the MILES trial led to FDA approval in 2015. LAM is diagnosed and managed at specialist centres.
Can I drink alcohol on Rapacan?
No specific alcohol interaction. Moderate intake is generally acceptable but alcohol worsens hyperlipidaemia (a common sirolimus side effect) and may interact with hepatic metabolism. If you have a transplanted liver or other hepatic disease, alcohol is contraindicated.
Medical disclaimer: This product page is for educational purposes and is not a substitute for medical advice. Immunosuppressants can cause life-threatening infections, malignancies, and birth defects. Use only under specialist supervision with appropriate monitoring.
More options in Anti Cancer Medication
Gerangschikt op recente bestelvolumes van MedsBase — wat andere klanten in deze categorie kiezen.
| Sterkte | 1 mg |
|---|---|
| Hoeveelheid | 30 Tablet/s, 60 Tablet/s, 90 Tablet/s |
| Farmaceutische vorm | Tablet/s |
| Fabrikant | Biocon Biopharmaceutical |
| Behandeling | Prevention of kidney transplant rejection |
| Generiek merk | Sirolimus |
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