SUMMARY  

• The OPSUMIT tablet is not scored nor has been evaluated for splitting.¹
• Physical characteristics, such as size, shape, and tablet score, can impact the uniformity of split tablets.² The decision to administer reformulated OPSUMIT (e.g., orally or via nasogastric tube) is at the discretion of the prescribing physician.
• NIOSH (National Institute for Occupational Safety and Health) published a guide to manage hazardous drug exposure in healthcare facilities, including hospitals, long-term care facilities, outpatient clinics, and nontraditional settings such as home healthcare.³
  • OPSUMIT was listed in the 2020 NIOSH Hazardous Drugs list as a developmental and/or reproductive hazard.⁴
• A stability study was conducted to evaluate the stability of crushed OPSUMIT film-coated tablets and crushed OPSUMIT film-coated tablets with either lactose or maize starch mixed in a 1:1 ratio, following storage for 4 weeks at 30°C-75% humidity.⁵
• A solubility study of the OPSUMIT film-coated tablet showed that >50% of the active ingredient was dissolved after 5 minutes and >90% after 45 minutes in 1000 mL of 50 mM sodium phosphate buffer (pH 6.8) with 0.1% (w/v) of cetyltrimethylammonium bromide (CTAB).⁶

CLINICAL DATA

Precautions for Handling OPSUMIT Tablets

The OPSUMIT tablet is not scored nor has been evaluated for splitting.¹ Physical characteristics, such as size, shape, and tablet score, can impact the uniformity of split tablets.² The decision to administer reformulated OPSUMIT (eg, orally or via nasogastric tube) is at the discretion of the prescribing physician.

NIOSH published a guide to manage hazardous drug exposure in healthcare facilities, including hospitals, long-term care facilities, outpatient clinics, and nontraditional settings such as home health.³ OPSUMIT was listed in the 2020 NIOSH Hazardous Drugs list as a developmental and/or reproductive hazard. It met the NIOSH criteria, but it does not have the manufacturer’s special handling information or is classified by the National Toxicology Program as “known to be a human carcinogen” or classified by the International Agency for Research on Cancer as “carcinogenic” or “probably carcinogenic”.⁴

Stability Information

A study evaluated the stability of crushed OPSUMIT film-coated tablets and crushed OPSUMIT film-coated tablets with either lactose or maize starch mixed in a 1:1 ratio, following storage for 4 weeks at 30°C-75% humidity. Study results showed no change in the appearance, macitentan content, or degradation products of crushed OPSUMIT tablets with/without lactose or maize starch after storage for 4 weeks at 30°C-75% humidity. Furthermore, the tablets were photostable after exposure to ultraviolet (UV) and visible light for 5 days.⁵

Solubility Information

During in vitro testing of the OPSUMIT film-coated tablet, >50% of the active ingredient was dissolved after 5 minutes and >90% after 45 minutes in 1000 mL of 50 mM sodium phosphate buffer (pH 6.8) with 0.1% (w/v) of CTAB.⁶

Literature Search

A literature search of MEDLINE^®, EMBASE^®, BIOSIS Previews^®, DERWENT^® (and/or other resources, including internal/external databases) was conducted on 29 March 2024.