Police allege the sophisticated syndicate involved two men buying drugs from an overseas supplier and selling them at a gym in Port Melbourne, with organised crime figures among hundreds of customers.
On Friday, two men aged 27 and 32 were arrested and multiple distribution centres uncovered.
Officers allege they contained millions of dollars worth of illegal steroids, other medication and more than $130,000 in cash.
Other searches at a Port Melbourne gym and Flemington home uncovered more illegal steroids.
The drug haul is so big, officers expected it would take two days to load the evidence into trucks and even more time to count the drugs and cash to determine the exact amount involved.
The two men have been hit with a string of charges including trafficking a commercial quantity of prescription medication, trafficking anabolic steroids and knowingly dealing with the proceeds of crime.
The pair were set to face the Melbourne Magistrates' Court on Saturday.
A 37-year-old Docklands woman was also arrested and charged with possessing methylamphetamine.
More people are expected to be charged.
Police in the ACT carried out other warrants on Friday and arrested a number of people allegedly involved in the operation.
Victoria Police Detective Inspector Patrick Watkinson said the bust should serve as a reminder that anyone who associates with organised crime figures in the slightest way would be found.
"The community may think dealing with performance-enhancing drugs is harmless but we're looking at the bigger picture here - which is to target all aspects of organised crime including the people associated with it," he said.
Det Insp Watkinson reminded people medication can only be supplied by accredited doctors and pharmacists, not personal trainers at a gym.
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