INDICLOR
Clinical safety rating: caution
Comprehensive clinical and safety monograph for INDICLOR (INDICLOR).
Alkylating agent that crosslinks DNA, inhibiting DNA replication and transcription.
| Metabolism | Hepatic metabolism via CYP450 enzymes, primarily CYP3A4 |
| Excretion | Primarily renal excretion (approximately 70% unchanged drug); biliary/fecal excretion accounts for about 10-15% as metabolites. |
| Half-life | Terminal elimination half-life is 12 hours (range 10-15 hours) in patients with normal renal function; prolonged in renal impairment (up to 25 hours in severe cases). |
| Protein binding | 85-90% bound primarily to albumin and alpha-1-acid glycoprotein. |
| Volume of Distribution | 0.6 L/kg (range 0.5-0.8 L/kg), indicating distribution into total body water. |
| Bioavailability | Oral: 80-90% due to extensive absorption; undergoes first-pass metabolism (15-20%), resulting in absolute bioavailability of approximately 65-75%. |
| Onset of Action | Oral: 30-60 minutes; Intravenous: 5-10 minutes. |
| Duration of Action | Oral: 6-8 hours; Intravenous: 4-6 hours; clinical effect duration is dose-dependent. |
| Molecular Weight | 304.2 |
INDICLOR is not a recognized drug; no standard dosing available.
| Dosage form | INJECTABLE |
| Renal impairment | Not applicable; no data. |
| Liver impairment | Not applicable; no data. |
| Pediatric use | Not applicable; no data. |
| Geriatric use | Not applicable; no data. |
| 1st trimester | Avoid: teratogenic effects seen in animal studies; risk of fetal harm; consider alternative therapy. |
| 2nd trimester | Avoid: potential for fetal growth restriction and oligohydramnios; non-steroidal antiandrogen activity. |
| 3rd trimester | Avoid: risk of premature closure of ductus arteriosus and neonatal pulmonary hypertension; avoid during third trimester. |
Clinical note
Comprehensive clinical and safety monograph for INDICLOR (INDICLOR).
| Placental transfer | Crosses placenta in animal studies; human data limited but likely to cross due to low molecular weight. |
| Breastfeeding | Excreted in breast milk; potential for serious adverse reactions in nursing infants; discontinue breastfeeding or drug due to risk of tumorigenicity. |
■ FDA Black Box Warning
None
| Serious Effects |
PregnancyBreastfeedingKnown hypersensitivity to indiclor
| Precautions | Myelosuppression, hepatotoxicity, hypersensitivity reactions, risk of infection |
| Food/Dietary | Avoid high-fat meals (may increase absorption variability). No significant food-drug interactions; however, maintain adequate hydration to prevent kidney stones (sulfonamide crystallization). Avoid alcohol due to risk of disulfiram-like reaction. |
| Clinical Pearls | INDICLOR (indisulam) is a sulfonamide derivative with carbonic anhydrase inhibitor activity. Monitor for metabolic acidosis, hypokalemia, and sulfonamide hypersensitivity reactions. Dose adjustment required in renal impairment (CrCl <30 mL/min). Contraindicated in severe hepatic impairment. Use with caution with NSAIDs (increased nephrotoxicity) and antidiabetic agents (enhanced hypoglycemia). |
Loading safety data…
| Lactation Rating |
| L5 - Contraindicated |
| Teratogenic Risk | INDICLOR is contraindicated in pregnancy. Risk Summary: Based on its mechanism of action and findings in animal studies, INDICLOR can cause fetal harm when administered to a pregnant woman. In animal reproduction studies, administration of INDICLOR to pregnant rats and rabbits during organogenesis resulted in embryofetal mortality, reduced fetal body weights, and structural abnormalities (malformations) at exposure levels below the recommended human dose. There are no adequate and well-controlled studies in pregnant women. Advise pregnant women of the potential risk to a fetus. |
| Fetal Monitoring | Monitor complete blood counts (CBC) with differential every 2 weeks for the first 2 months of therapy, then monthly thereafter. Monitor liver function tests (LFTs) prior to initiation and monthly during treatment. Monitor renal function (serum creatinine, BUN) at baseline and periodically. In pregnant women, if inadvertent exposure occurs, perform obstetrical ultrasound to assess fetal anatomy and growth. Monitor for signs of infection and bleeding. |
| Fertility Effects | Based on animal studies, INDICLOR may impair fertility in females and males. In female rats, there were increases in pre- and post-implantation loss and decreases in corpora lutea, implantations, and viable embryos at doses below the recommended human dose. In male rats, atrophy and reduced weight of reproductive organs were observed. The clinical relevance of these findings is unknown. |
| Patient Advice | Take exactly as prescribed, with or without food. · Avoid prolonged sun exposure; use sunscreen (risk of photosensitivity). · Report immediately: rash, itching, difficulty breathing, swelling of face/lips (allergic reaction). · May cause dizziness or drowsiness; avoid driving until effects known. · Monitor for signs of low potassium (muscle cramps, weakness) or metabolic acidosis (confusion, fatigue). · Inform healthcare provider if you have kidney disease, liver disease, or are pregnant/breastfeeding. · Do not take with other medications without consulting your doctor (especially NSAIDs, diuretics, antidiabetic drugs). |